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Antibacterial Chemical Compounds

                                                                                                                                                                                                                                  Download data

ENTITY POTENCY SAFETY INFORMATION EVIDENCE PMID
(Z)-N-benzylidene-2-(tert-butoxycarbonylamino)-1-(5-iodo-1H-indol-3-yl)ethanamine oxidefourfold decrease of the ciprofloxacin minimum inhibitory concentration against the SA-1199B strain when used at a concentration of 0.5 mg L(-1)1-(1H-indol-3-yl)ethanamine derivatives as potent Staphylococcus aureus NorA efflux pump inhibitors.24677763
13-Deoxytetrodecamycin (WAC04657)Potent bioactivity against Gram-positive pathogens including multidrug-resistant Staphylococcus aureus and Gram-negative pathogens13-Deoxytetrodecamycin has potent bioactivity against Gram-positive pathogens including multidrug-resistant Staphylococcus aureus.26014719
3'-bromo-3'-deoxy-arabinofuranosylthymine (33)MIC(50) = 1 microg/mL against wild-type M. tuberculosis strain (H37Ra) and 1-2 microg/mL against rifampicin-resistant and isoniazid-resistant) strains of M. tuberculosisNo cytotoxicity was found up to the highest concentration of compounds tested (CC(50) > 100-200 microg/mL) against a human cell line3'-bromo analogues of pyrimidine nucleosides as a new class of potent inhibitors of Mycobacterium tuberculosis. T20420370
thiosemicarbazide intermediatesthiosemicarbazide intermediates in the syntheses of these compounds are also moderately potent inhibitors of the IMP-1 MBL (metallo-?-lactamases) from Pseudomonas aeruginosaNA3-mercapto-1,2,4-triazoles and N-acylated thiosemicarbazides as metallo-?-lactamase inhibitors. The production of ?-lactamases is an effective strategy by which pathogenic bacteria can develop resistance against ?-lactam antibiotics.22115595
4-(3-Chloro-5-(trifluoromethyl)pyridin-2-yl)-N-(4-methoxypyridin-2-yl)piperazine- 1-carbothioamide (ML267)exhibit submicromolar inhibition of bacterial Sfp-PPTase with no activity toward the human orthologue4-(3-Chloro-5-(trifluoromethyl)pyridin-2-yl)-N-(4-methoxypyridin-2-yl)piperazine- 1-carbothioamide (ML267), a potent inhibitor of bacterial phosphopantetheinyl transferase that attenuates secondary metabolism and thwarts bacterial growth.24450337
4-Aminoquinolone piperidine amides (AQs)potent DprE1 inhibition (IC50 < 10 nM) along with potent cellular activity (MIC = 60 nM) against Mtb4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.24871036
6 beta-Iodopenicillanic acid (UI-38,006)Active against beta-lactamase-producing strains of Staphylococcus aureus, Haemophilus influenzae, Bacteroides fragilis.6 beta-Iodopenicillanic acid (UI-38,006), a beta-lactamase inhibitor that extends the antibacterial spectrum of beta-lactam compounds: initial bacteriological characterizationUK-38,006, 6 beta-iodopenicillanic acid, was shown to be a potent inhibitor of beta-lactamase enzymes.6272628
poly-D-lysine-Le(b) hexasaccharide and an Le(b) human serum albumin conjugateinhibited adherence of H. pylori to gastric epithelium and displaced adherent bacteria when added to human stomach sectionsA human domain antibody and Lewis b glycoconjugate that inhibit binding of Helicobacter pylori to Lewis b receptor and adhesion to human gastric epithelium19832116
Nitrofuranylamides (NFAs)Highly active against drug-susceptible and -resistant strains of M. tuberculosis, with MICs 0.0004-0.05 mg/LA microbiological assessment of novel nitrofuranylamides as anti-tuberculosis agents18693235
bispecific antibody BiS4effective against Pseudomonas aeruginosaA multifunctional bispecific antibody protects against Pseudomonas aeruginosa. Widespread drug resistance due to empiric use of broad-spectrum antibiotics has stimulated development of bacteria-specific strategies for prophylaxis and therapy based on modern monoclonal antibody (mAb) technologies.25391481
aryl isonitrile analogs(MIC, in ?M) of isonitrile compounds, against methicillin-sensitive (MSSA) and methicillin-resistant Staphylococcus aureus (MRSA) strains rnge 2 - >128 in ?M. The most potent antibacterial aryl isonitrile analogs (MIC 2 ?M) did not show any toxicity against mammalian cells up to a concentration of 64 ?M.A new class of compounds featuring an aryl isonitrile moiety has been discovered that exhibits potent inhibitory activity against several clinically-relevant MRSA and VRSA isolates.26164843
ketolides prepared with the (R)-alkyl group, compound 5p with an N-(3-quinoxalin-6-yl-propyl)-propionamide moietypotent in vitro antibacterial activities against the key respiratory pathogens including Haemophilus influenzae and erythromycin-resistant S. pneumoniaeA new type of ketolide bearing an N-aryl-alkyl acetamide moiety at the C-9 iminoether: synthesis and structure-activity relationships16460944
6-Benzyl Ether BenzoxaboroleMIC 2 ?Mno cytotoxicity against eukaryotic cellsA Novel 6-Benzyl Ether Benzoxaborole Is Active against Mycobacterium tuberculosis In Vitro. We identified a novel 6-benzyl ether benzoxaborole with potent activity against Mycobacterium tuberculosis28674058
6-O-substituted 8a-aza-8a-homoerythromycin A 3-O-acylidesActivity against Haemophilus influenzae and constitutively MLSB-resistant strains of Streptococcus pneumoniae and Streptococcus pyogenesA novel series of 6-O-substituted 8a-aza-8a-homoerythromycin A 3-O-acylides has been discovered with potent activity against key respiratory pathogens, including those inducibly and constitutively resistant to erythromycin.27657812
6,9:11,12-dicarbonate acylide 47 (FMA0122) and 11,12-carbamate acylide 19 (TEA0929)Activity against almost all gram positive and negative pathogensA novel series of acylides, 3-O-(aryl)acetylerythromycin A derivatives, were synthesized and evaluated.12801234
1beta-methyl-2-(5-substituted thiazolo pyrrolidin-3-ylthio)carbapenem derivativesActivities against both Gram-positive including MRSA and Gram-negative bacteria , compound 28c having 4'-amide substituted thiazole moiety is most potentA particular compound (28c) having 4'-amide substituted thiazole moiety showed the most potent antibacterial activity.12350291
7beta-[2-(5-amino-1,2,4-thiadiazol-3-yl)-2(Z)-ethoxyiminoacetamido]-3-[1-(3-methy laminopropyl)-1H-imidazo[4,5-b]pyridinium-4-yl]methyl-3-cephem-4-carboxylate sulfate (S-3578)activity against both gram-positive bacteria including methicillin-resistant Staphylococcus aureus (MRSA) and gram-negative bacteria including Pseudomonas aeruginosaA series of 7-aminothiadiazolylcephalosporins having a 1-(substituted)-1H-imidazo[4,5-b]pyridinium group at the C-3' position of the cephem nucleus were synthesized and evaluated for in vitro antibacterial activities.12546419
1-cyclopropyl-6-fluoro-1, 4-dihydro-5-methyl-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxyli c acid hydrochloride (grepafloxacin)in vitro antibacterial activity against Streptococcus pneumoniae and high in vivo efficacy on the experimental systemic infections caused by the Gram-positive and -negative bacteria tested.A series of substituted 1-cyclopropyl-6-fluoro-1, 4-dihydro-5-methyl-4-oxo-3-quinoline carboxylic acids was synthesized and tested for their in vitro and in vivo antibacterial activity.8770395
ABT773(MIC-90=0.03 mg/l) against the staphylococci , MIC-90 range: <0.0075-0.5mg/l against Streptococcus pneumoniae, S. pyogenes and S. agalactiae irrespective of their antibiotic resistance phenotype.ABT773 displays the characteristics of a promising agent that deserves to be introduced as the empirical therapy of infections caused by the bacterial species tested here, even if they are multiply resistant.14732308
AFN-1252Maximum reductions in viable count against MSSA 29213 and MRSA S186 were approximately 4 logs, achieved by 450 mg q12h (fAUC/MIC = 1875) dosing at 28 hoursActivity of AFN-1252, a novel FabI inhibitor, against Staphylococcus aureus in an in vitro pharmacodynamic model simulating human pharmacokinetics.23433442
Debio1452 (previously AFN-1252)The MIC50s for MSSA, MRSA, and molecularly characterized MRSA strains were 0.004 ?g/ml, and the MIC90s ranged from 0.008 to 0.03 ?g/ml. Fot coagulase-negative staphylococci (CoNS) MIC50/90, 0.015/0.12 ?g/mlActivity of Debio1452, a FabI inhibitor with potent activity against Staphylococcus aureus and coagulase-negative Staphylococcus spp., including multidrug-resistant strains. Staphylococcus aureus and coagulase-negative staphylococci25691627
BAL19403, novel macrolidePotent activity against propionibacteria in vitro, >10-fold higher activity than erythromycinActivity of the novel macrolide BAL19403 against ribosomes from erythromycin-resistant Propionibacterium acnes.17923495
PYRRO-C3D, cephalosporin-3-diazeniumdiolate nitric oxide (NO) donor prodruga log fold reduction (10-fold reduction or 1-log-unit reduction) in viability (P < 0.05) relative to azithromycin alone.Adjunctive therapy with NO mediated through PYRRO-C3D represents a promising approach for reducing biofilm-associated antibiotic tolerance.27919896
aerosolized colistin sodiumThe mean time to spontaneous emergence of sensitive organisms was 144.6+/-48.0 days in candidates who did not use colistin sodium and was significantly longer than in the candidates who used colistin sodium (P=0.007).Aerosolized colistin sodium may be a useful therapy to promote emergence of sensitive microbes in CF candidates with pan-resistant isolates of Pseudomonas.9311714
1,4-naphthoquinonesThe EC50 was 8 microg/ml for 5-amino-8-hydroxy-1,4-naphthoquinone against S. aureus, S. intermedius, and S. epidermidis.An effective in vitro activity of 5-amino-8-hydroxy-1,4-naphthoquinone and encourage further studies for its application in antibiotic therapy.12131921
3'-azido-3'-deoxythymidine (BW A509U).potent bactericidal activity against many members of the family Enterobacteriaceae, including strains of Escherichia coli, Salmonella typhimurium, Klebsiella pneumoniae, Shigella flexneri, and Enterobacter aerogenesAntibacterial activity and mechanism of action of 3'-azido-3'-deoxythymidine (BW A509U). The thymidine analog 3'-azido-3'-deoxythymidine (BW A509U; azidothymidine [AZT]) had potent bactericidal activity against many members of the family Enterobacteriaceae, including strains of Escherichia coli, Salmonella typhimurium, Klebsiella pneumoniae, Shigella flexneri, and Enterobacter aerogenes.3551832
2-(2',4'-Dibromophenoxy)-4,6-dibromophenolMIC range was 0.117-2.5 microg/mL against all the Gram positive bacteria and 0.5-2 microg/mL against Gram negative bacteriaAntibacterial activity of 2-(2',4'-dibromophenoxy)-4,6-dibromophenol from Dysidea granulosa.19841726
7beta-[2-(5-amino-1,2,4-thiadiazol-3-yl)-2(Z)-cyclopentyloxyiminoacetamido]-3-(3, 6-diaminoimidazo[1,2-b]pyridazinium-1-yl)methyl-3-cephem-4-carboxylateIC50 = 1.6 microg/ml for penicillin binding protein 2' (PBP2'Antibacterial Activity of 7?-[2-(5-Amino-1, 2, 4-thiadiazol-3-yl)-2(Z)-alkoxyiminoacetamido]-3-(substituted imidazo[1, 2-b]pyridazinium-1-yl)methyl-3-cephem-4-carboxylates and Related Compounds11132951
AM-1155, a novel fluoroquinoloneFor experimental murine pneumonia with S. pneumoniae intermediately resistant to penicillin, oral administration of AM-1155 showed efficacy higher than that of levofloxacin and equal to that of sparfloxacin.Antibacterial activity of AM-1155 against penicillin-resistant Streptococcus pneumoniae. AM-1155, a novel fluoroquinolone, exhibited potent activity against Streptococcus pneumoniae, including penicillin-resistant strains; the MIC90 for 48 clinical isolates was 0.25 mg/L.9511043
1,13-bis{[(2,2-diphenyl)-1-ethyl]thioureido}-4,10-diazatridecaneBactericidal activity, primarily by depolarization of the cytoplasmic membrane and permeabilization of the bacterial outer membrane.limited adverse effects against the HEK293T human kidney embryonic cells and A549 human adenocarcinoma cellsAntibacterial Diamines Targeting Bacterial Membranes.26964758
ether derivative ?-artecyclopropylmetherExhibited MIC range, MIC(90), and minimum bactericidal concentration range values of 0.25 to 1.0 ?g/ml, 1.0 ?g/ml, and 1 to 16 ?g/ml, respectively, against both resistant and sensitive strains of H. pylori.Anti-Helicobacter pylori potential of artemisinin and its derivatives22687518
Ceragenins CSA-8 and CSA-13, cationic steroid moleculesActivities against clinical isolates of vancomycin-intermediate S. aureus (VISA), heterogeneous vancomycin-intermediate S. aureus (hVISA), as well as vancomycin-resistant S. aureus (VRSA)Antimicrobial activities of ceragenins against clinical isolates of resistant Staphylococcus aureus. The rise in the rates of glycopeptide resistance among Staphylococcus aureus isolates is concerning and underscores the need for the development of novel potent compounds.17210765
PD127391 (CI-960 and AM-1091) and PD131628, new quinolonesPD127391 MIC90, 2 micrograms/ml and PD131628 MIC90 greater than 8 micrograms/ml against Bacteroides fragilis; PD127391 MIC90s, 0.015-1.0 micrograms/ml and PD131628 MIC90s, 0.03 - greater than 8 micrograms/ml against Gram-positive organisms.Antimicrobial activity evaluations of two new quinolones, PD127391 (CI-960 and AM-1091) and PD131628.1665774
BC-3781, pleuromutilin compoundBC-3781 exhibited potent activity against methicillin-resistant Staphylococcus aureus (MIC(50/90), 0.12/0.25 ?g/ml), coagulase-negative staphylococci (MIC(50/90), 0.06/0.12 ?g/ml), ?-hemolytic streptococci (MIC(50/90), 0.03/0.06 ?g/ml), viridans group streptococci (MIC(50/90), 0.12/0.5 ?g/ml), and Enterococcus faecium (including vancomycin-nonsusceptible strains) (MIC(50/90), 0.12/2 ?g/ml).Antimicrobial activity of the investigational pleuromutilin compound BC-3781 tested against Gram-positive organisms commonly associated with acute bacterial skin and skin structure infections22232289
RLP068/ClQuantitative CLSM studies showed a reduction in biofilm biomass (biofilm disruption) and a decrease in viable cell numbers, as determined by standard plate counting, in the S. aureus and P. aeruginosa biofilms exposed to APDT with the photosensitiser RLP068/Cl.Antimicrobial photodynamic therapy (APDT), a non-antibiotic broad-spectrum antimicrobial treatment, is also active against multidrug-resistant micro-organisms such as meticillin-resistant Staphylococcus aureus (MRSA) and Pseudomonas aeruginosa.24933446
1-tert-butyl-1,4-dihydro-7-(4,4-dimethyloxazolidin-3-yl)-6-nitro-4-oxo-1,8-naphth yridine-3-carboxylic acid (10q)MIC of 0.1 microM against MTB and MDR-TBAntimycobacterial activities of novel 1-(cyclopropyl/tert-butyl/4-fluorophenyl)-1,4-dihydro- 6-nitro-4-oxo-7-(substituted secondary amino)-1,8-naphthyridine-3-carboxylic acid17960928
ceruleninMICs ranging from 1.5 to 12.5 mg/L against Mycobacterial species, inhibition of fatty acid synthesisAntimycobacterial activity of cerulenin and its effects on lipid biosynthesis.11252327
2-isonicotinoyl-N-[2-(trifluoromethyl)phenyl]hydrazinecarbothioamide (4i)Minimum inhibitory concentration of 0.58 microM against M. tuberculosis H(37)R(v) and INH resistant M. tuberculosisAntimycobacterial activity of novel N-(substituted)-2-isonicotinoylhydrazinocarbothioamide endowed with high activity towards isoniazid resistant tuberculosis.18343086
TD-1792, a multivalent glycopeptide-cephalosporinpotent bactericidal activity at ? 0.12 ?g/ml, highly active against methicillin-susceptible S. aureus (MIC(90), 0.015 ?g/ml), methicillin-resistant S. aureus, and heterogeneous vancomycin-intermediate S. aureus (MIC(90), 0.03 ?g/ml)Antistaphylococcal activity of TD-1792, a multivalent glycopeptide-cephalosporin antibiotic.22203585
PlakofuranolactoneThe quorum quenching activity of plakofuranolactone was evaluated using reporter gene assays for long- and short-chain signals (E. coli pSB1075, E. coli pSB401, and C. violeaceum CV026) and was confirmed by measuring the total protease activity (a virulence factor which is under control of the LasI/R system) of the wild-type P. aeruginosa PAO1.As an alternative to the classic antibiotic therapy, attenuation of the bacteria virulence affecting their Quorum sensing (QS) system is a promising approach. A new ?-lactone that is capable of inhibiting the LasI/R QS system, plakofuranolactone (1), was discovered in the extract of the marine sponge Plakortis cf. lita, and its structure, including absolute configuration, was determined by NMR spectroscopy, MS spectrometry, and quantum-mechanical prediction of optical rotation.28264490
Auranofin and N-heterocyclic carbene gold-analogsAuranofin completely inhibited H. pylori growth at 1.2 ?M, gold(I)-N-heterocyclic carbene compounds has MICs against H. pylori (2 ?M)lower toxicities for human embryonic kidney cells (HEK-293T cells)Auranofin and N-heterocyclic carbene gold-analogs are potent inhibitors of the bacteria Helicobacter pylori. Auranofin is an FDA-approved gold-containing compound used for the treatment of rheumatoid arthritis.27279627
AZ6142, bacterial topoisomerase inhibitorsinhibits both type II topoisomerases in S. aureus but that DNA gyrase is the primary targetAZ6142 has very potent activity against Gram-positive organisms, including Staphylococcus aureus, Streptococcus pneumoniae, and Streptococcus pyogenes.26077256
ABT-773, a new ketolideActivity against macrolide-susceptible and -resistant S. pneumoniaeBactericidal effect and pharmacodynamics of cethromycin (ABT-773) in a murine pneumococcal pneumonia model.12234843
BAL30072, a novel siderophore sulfactamThe MIC(90)s were 4 microg/ml for MDR Acinetobacter spp. and 8 microg/ml for MDR P. aeruginosa, whereas the MIC(90) of meropenem for the same sets of isolates was >32 microg/ml.BAL30072 showed potent activity against multidrug-resistant (MDR) Pseudomonas aeruginosa and Acinetobacter sp. isolates, including many carbapenem-resistant strains.20308379
nitrobenzotrifluoride-containing ohydroxybenzylamine derivatives (3a-3x)FabH inhibitors, inhibitory potency against the aminoacylation of S. aureus tyrosyl-tRNA synthetaseBased on our previous findings that o-hydroxybenzylamine derivatives demonstrated potent FabH inhibitory and antimicrobial activities, computer-assistant drug design was introduced and then a series of novel nitrobenzotrifluoride-containing ohydroxybenzylamine derivatives (3a-3x) was designed and synthesized.25219926
chimeric protein containing human FH domains 6 and 7 fused to human IgG1 Fc (FH6,7/HuFc)At 8 to 9 h after the challenge, the FH6,7/HuFc-treated rats had >100-fold fewer CFU per ml of blood than control animals pretreated with phosphate-buffered saline (PBS) or FH18-20/HuFc, which does not bind to meningococci (P < 0.0001).Because many microbes share a common binding region(s) in FH, FH/Fc chimeric proteins may be a promising candidate for adjunctive therapy against drug-resistant pathogens. Copyright ? 2014, American Society for Microbiology.25143339
Benzoyl peroxideBenzoyl peroxide may have underappreciated potential to treat noninflammatory acne as monotherapy or in combination with a topical retinoid, an important antibiotic-sparing strategy.19202772
benzoyl peroxidereduce total P acnes count by 99.7%Benzoyl peroxide works rapidly on P acnes without causing antibiotic resistance.23839205
Combination of Tobramycin and bicarbonateBicarbonate synergises with tobramycin to enhance killing of planktonic bacteria.28721244
dipyridinium-based cationic amphiphile (compound 1) and compound 1-loaded nanocarrierAnti-biofilm activity on Staphylococcus aureus MTCC 96 and Pseudomonas aeruginosa MTCC 2488Biocompatible nanocarrier fortified with a dipyridinium-based amphiphile for eradication of biofilm.25162678
9H-isothiazolo[5,4-b]quinoline-3,4-diones containing heteroaromatic groups at the 7-positionPotent antistaphylococcal activity (MICs 2 microg/mL) against a multi-drug-resistant strain (ATCC 700699)low cytotoxic activity (CC(50)>100 microM) against the human cell line Hep2 (laryngeal carcinoma)Biological evaluation of isothiazoloquinolones containing aromatic heterocycles at the 7-position: In vitro activity of a series of potent antibacterial agents that are effective against methicillin-resistant Staphylococcus aureus.16337789
dicationic bis-benzimidazolesin vitro antibacterial activities, including drug-resistant bacterial strainsBis-benzimidazole diamidine compounds have potential for further investigation as a new class of potent anti-MRSA and anti-VRE agents.19208475
bis-cyclic guanidine compoundsin vitro potency against C. difficile UK6 with MIC values of 1.0 ?g mL-1.cytotoxic selectivity index (SI) values up to 37Bis-Cyclic Guanidines as a Novel Class of Compounds Potent against Clostridium difficile.29768720
Blockade of the susceptible position led to the discovery of the first antivirulence compound that is potent in vivo and targets PqsR, thus providing a proof of concept for this novel antivirulence therapy. Copyright ? 2014 WILEY-VCH Verlag GmbH & Co.24338917
BMS-284756 is a novel des-fluoro(6) quinolone30 mg/kg as a single or divided doseBMS-284756 is a novel des-fluoro(6) quinolone with a broad antimicrobial activity, including Streptococcus pneumoniae. The bactericidal effect of BMS-284756 in CSF was concentration dependent.11600362
2-thiopyridine derivativeseffective against both active and dormant M. tuberculosis cellsBy means of the model of M. tuberculosis nonculturability, several new 2-thiopyridine derivatives were found to have potent antitubercular activity.24126578
Carbon-carbon-linked (pyrazolylphenyl)oxazolidinonesalpha-N-substituted methyl pyrazole (10alpha): MICs Carbon-carbon-linked (pyrazolylphenyl)oxazolidinones with antibacterial activity against multiple drug resistant gram-positive and fastidious gram-negative bacteria.11711300
Cathodic voltage-controlled electrical stimulation of titaniumCathodic voltage-controlled electrical stimulation of titanium for prevention of methicillin-resistant Staphylococcus aureus and Acinetobacter baumannii biofilm infections27890730
CefiderocolMIC against Escherichia coli ATCC 25922 (0.06-0.5 ?g/mL) and Pseudomonas aeruginosa ATCC 27853 (0.06-0.5 ?g/mL).Cefiderocol (formerly S-649266) is a new catechol-substituted parenteral siderophore cephalosporin with potent in vitro antibacterial activity against Gram-negative isolates including multidrug-resistant strains.28410852
CG400462MIC(90) was 0.5 microg/mL against 238 strains of Staphylococcus aureus and 1.0 microg/mL against 51 strains of coagulase-negative methicillin-susceptible or -resistant staphylococciCG400462, a new bacterial enoyl-acyl carrier protein reductase (FabI) inhibitor. CG400462, a novel FabI inhibitor, has a potent antibacterial activity against staphylococci.17723291
N2,N4-Disubstituted Quinazoline-2,4-Diamines with 6-position is replaced with a halide or an alkyl substituentMICs 0.5 ?M against multidrug-resistant A. baumanniiCharacterizing the Antimicrobial Activity of N2,N4-Disubstituted Quinazoline-2,4-Diamines toward Multidrug-Resistant Acinetobacter baumannii.28289036
N-(2-hydroxypropyl)-3-trimethylammonium chitosan chlorides (HTCC)Bacteria and fungi (MIC = 125-250 ?g/mL). In a murine model of superficial skin infection - (3.2 log MRSA reduction at 100 mg/kg) with no to minimal inflammation.Chitosan Derivatives Active against Multidrug-Resistant Bacteria and Pathogenic Fungi: In Vivo Evaluation as Topical Antimicrobials. The continuous rise of antimicrobial resistance and the dearth of new antibiotics in the clinical pipeline raise an urgent call for the development of potent antimicrobial agents.27589087
CitrininPotent antibacterial activity against methicillin-resistant Staphylococcus aureus (S. aureus), rifampicin-resistant S. aureus, wild type S. aureus and vancomycin-resistant Enterococcus faecium with MICs of 3.90, 0.97, 1.95 and 7.81 ?g/mL, respectively.Citrinin (1) is reported from sponge associated Penicillium sp. from this study and for its strong antibacterial activity against multi-drug resistant human pathogens including cytotoxicity against brine shrimp larvae, which indicated that sponge associated Penicillium spp. are promising sources of natural bioactive metabolites23620853
poly(methyl methacrylate) (PMMA)Collectively, our in vitro results indicate that PMMA is a more suitable carrier compared to CaSO4 for delivery of Ga(NO3)3; moreover they provide evidence for the potential use of Ga(NO3)3 with PMMA as a strategy for the prevention and/or treatment for orthopaedic infections.26885514
Combination of pantothenamides with vanin inhibitorsa series of pantetheinase inhibitors based on a pantothenate scaffold that inhibited serum pantetheinase activity in the nanomolar range was synthesizedCombination of pantothenamides with vanin inhibitors as a novel antibiotic strategy against gram-positive bacteria.23877685
TXA709This synergy reduces the dose of TXA709 required for efficacy 3-foldCombining the FtsZ-Targeting Prodrug TXA709 and the Cephalosporin Cefdinir Confers Synergy and Reduces the Frequency of Resistance in Methicillin-Resistant Staphylococcus aureus. Combination therapy of bacterial infections with synergistic drug partners offers distinct advantages over monotherapy.27161635
Myrtacine(?)Antibiofilm activity against Propionibacterium acnesCONCLUSION: The efficiency of Myrtacine(?) New Generation on P. acnes biofilm alone or combined with antibiotics was demonstrated and can lead to consider it as a potent adjunctive product efficient during the antibiotic course for acne vulgaris treatment.26969384
IFNG1 ? 106 IU of human recombinant IFN gamma or placebo intramuscularly, daily during 4 weeks and then 3 times per week for the next 20 weeks.No severe events were recorded.CONCLUSION: These data suggest that IFN gamma is useful and well tolerated as adjuvant therapy in patients with pulmonary atypical Mycobacteriosis, predominantly MAC.18267006
E-101 Solution is composed of porcine myeloperoxidase (pMPO), glucose oxidase, glucose as the substrate and specific amino acids in an aqueous vehicle.E-101 showed MIC(90) values of 0.03, 0.5 and 0.5 mg pMPO/L for staphylococci (n = 140), streptococci (n = 95) and enterococci (n = 55), respectively. MIC(90) values ranged between 0.03-0.5 and ? 0.004-0.12 mg pMPO/L for Enterobacteriaceae (n = 148) and Gram-negative non-Enterobacteriaceae (n = 92) strains, respectively. There was no antimicrobial tolerance to E-101 for Staphylococcus aureus, Streptococcus agalactiae or Streptococcus pyogenes.Conclusions E-101 shows potent and broad-spectrum in vitro activity against bacteria that are the causative pathogens of SSIs, thereby providing the impetus to test its clinical utility in the prevention of SSIs.21118915
ACHN-490, a sisomicin derivativeActive at ? 2 mg/L against all tested isolates with carbapenem resistance mechanisms other than NDM enzyme, mostly with MICs of 0.12-0.5 mg/LCONCLUSIONS: ACHN-490 has potent activity versus carbapenem-resistant isolates, except those also harbouring 16S rRNA methylases; isepamicin is also widely active, though less potent than ACHN-490.21078604
CG400549FabI inhibitor, MIC90 0.25 mg/L against clinical isolates of S. aureus, and 1 mg/L against clinical isolates of coagulase-negative staphylococciCONCLUSIONS: CG400549 had potent in vitro and in vivo activity against staphylococci, including methicillin-, ciprofloxacin- and multidrug-resistant staphylococci strains.17606482
platelet-rich plasma (PRP)When compared to control group, PRP and PPP significantly suppressed bacterial growth of MRSA, K. pneumoniae, and P. aeruginosa at 1st, 2nd, 5th, and 10th hours of incubation (p < 0.05).CONCLUSIONS: Emerging PRP and other platelet-derived products seem to be promising alternative tools besides antibiotic treatment, debridement, negative pressure wound therapy, hyperbaric oxygen therapy, and other treatment options for treating diabetic foot infections. DOI: 10.1007/s00068-018-0957-029700554
isothiazolone compound REDX04957 and its enantiomers (REDX05967 and REDX05990)activity against the ESKAPE organisms, except of Enterococcus spp and quinolone-resistant strains harbouring GyrA S83L and D87G mutations (MIC ?4 mg/L)lack of cytotoxicity against HepG2 cells at 128 mg/LCONCLUSIONS: Isothiazolone compounds show potent activity against Gram-positive and -negative pathogens with a dual targeting mechanism-of-action and a low potential for resistance development, meriting their continued investigation as broad-spectrum antibacterial agents.27353465
LytA lytic enzymeIn the time-kill assays, after 5 h of exposure to LytA, Cpl-1 or Pal, the mean differences in colony counts versus controls were -3.55, -2.66 and -2.71 log(10) cfu/mL, respectively.CONCLUSIONS: LytA, Cpl-1 or Pal, alone or in combination, might prove to be effective in combination therapy, as well as in monotherapy against S. pneumoniae.17827138
Conjugation of the N5-acetyl-N5-hydroxy-L-ornithine tripeptide and the bis(catechol) siderophore to the potent carbacephalosporinantibacterial activity against E. coli X580Conjugation of the N5-acetyl-N5-hydroxy-L-ornithine tripeptide and the bis(catechol) siderophore to the potent carbacephalosporin loracarbef and closely related analogs provided compounds which exhibited antibacterial activity against E. coli X580.1503447
(E)-3-(2-1H-benzo[d]imidazol-1-yl)-1-((4-chlorobenzyl)oxy)imino)ethyl)-2H-chromen -2-onebroad spectrum antibacterial activity against Pseudomonas aeruginosa, Staphylococcus aureus, Bacillus subtilis and Proteus vulgarisno cytotoxicity and hemolysis at 10 times the MIC concentrationCoumarin-benzimidazole hybrids as a potent antimicrobial agent: synthesis and biological elevation. Molecular hybridization approach is an emerging tool in drug discovery for designing new pharmacophores with biological activity.28634338
1beta-methylcarbapenems bearing an (imidazo[5,1-b]thiazolium-6-yl)methyl moiety, a 5,5-fused heterobicycle, at the C-2 position (CP0569)potent antibacterial activities against Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA), and Gram-negative bacteria, including Pseudomonas aeruginosaCP0569 (1r) and its analogues showed potent antibacterial activities against Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA), and Gram-negative bacteria, including Pseudomonas aeruginosa.12878141
cephalosporins bearing a 5,5-fused ring system, an (imidazo[5,1-b]thiazolium-6-yl)methyl group, at the C-3 positionpotent antibacterial activity against Pseudomonas aeruginosa and MRSACP6679 (1s) and its analogues showed potent antibacterial activities against gram-positive and gram-negative bacteria, including Pseudomonas aeruginosa.11131169
fursultiamine hydrochloride (FTH)FTH has no cytotoxic effects on either host cells or pathogen at the tested concentrations.Current study validated the antivirulence strategy targeting the HlyU virulence transcription factor and toxin-network of V. vulnificus and demonstrated that FTH, exhibits a potential to inhibit the pathogenesis of deadly, opportunistic human pathogen, V. vulnificus without inducing AMR.29868508
CW-270033, a novel pyrrolidinyl-thio carbapenemPotent in-vivo activity against E. coli ATCC 25922, P. aeruginosa ATCC 27853, and S. aureus SMITHCW-270033, a novel pyrrolidinyl-thio carbapenem, has potent antimicrobial activity in vitro and in vivo17329859
Cyclothialidine (1, Ro 09-1437) modified structuresThe best activities were displayed by 14-membered lactones, and representatives of this subclass exhibit excellent and broad in vitro antibacterial activity against Gram-positive pathogens, including Staphylococcus aureus, Streptococcus pyogenes, and Enterococcus faecalis, and overcome resistance against clinically used drugs.Cyclothialidine (1, Ro 09-1437) is a potent DNA gyrase inhibitor that was isolated from Streptomyces filipinensis NR0484 and is a member of a new family of natural products.14998336
3-methoxybenzamide derivativesMost potent compound had average MIC of 0.12 ?g/ml against all staphylococcal species, including methicillin- and multidrug-resistant Staphylococcus aureus and Staphylococcus epidermidisDerivatives of 3-methoxybenzamide, including compound PC190723, have been reported to be potent and selective antistaphylococcal agents which exert their effects through the disruption of intracellular FtsZ function.23114779
N-3,5-bis(trifluoromethyl)phenyl-3,5-dichlorobenzenesulfonanilide (16b), and 3,5-bis(trifluoromethyl)-N-(3,5-dichlorophenyl)benzenesulfonanilide (16c)compound 16b has [MIC=0.5microg/mL (MRSA), 1.0microg/mL (VRE)], and compound 16c has [MIC=0.5microg/mL (MRSA), 1.0microg/mL (VRE)]Design and synthesis of benzenesulfonanilides active against methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus18468909
fluorine-substituted chalcone analogsPotent antimicrobial (tuberculosis and other pathogenic bacteria) and antifungal actifunal activityDesign of potent fluoro-substituted chalcones as antimicrobial agents.28118738
coumarin-chalcone derivativesAntibacterial activity against Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, and marine pathogen Tenacibaculum maritimum, responsible for tenacibaculosis in fish,Design, synthesis and antibacterial study of new potent and selective coumarin-chalcone derivatives for the treatment of tenacibaculosis.26433630
ampicillin-tetramic acid hybrid antibioticsDesign, synthesis and microbiological evaluation of ampicillin-tetramic acid hybrid antibiotics. Exploiting iron-uptake pathways by conjugating ?-lactam antibiotics with iron-chelators, such as catechol and hydroxamic acid is a proven strategy to overcome permeability-related resistance in Gram-negative bacteria.27189120
6-O-arylpropargyl diazalidespotent activity against erythromycin-resistant respiratory tract pathogensDesign, synthesis and structure-activity relationships of 6-O-arylpropargyl diazalides with potent activity against multidrug-resistant Streptococcus pneumoniae. A novel series of 6-O-arylpropargyl diazalides was synthesized and evaluated for their antibacterial activity.15863336
neomycin-C16 and neomycin-C20 conjugates (aminoglycoside-lipid conjugates)The MIC of neomycin-C16 (C20) conjugates against methicillin-resistant Staphylococcus aureus (MRSA) is comparable to clinically used antiseptics.Design, synthesis, and antibacterial activities of neomycin-lipid conjugates: polycationic lipids with potent gram-positive activity18778047
N-(6-phenylheptyl)demethylvancomycin (12 a)~18-fold more efficacious than vancomycin against MRSADesign, synthesis, and antibacterial activity of demethylvancomycin analogues against drug-resistant bacteria23576378
NO(2) (o) substituted 3-benzofuran-5-aryl-1-pyrazolylcarbonyl-4-oxo-naphthyridinpotent activity against Mycobacterium tuberculosisDesign, synthesis, and antitubercular evaluation of novel series of 3-benzofuran-5-aryl-1-pyrazolyl-pyridylmethanone and 3-benzofuran-5-aryl-1-pyrazolylcarbonyl-4-oxo-naphthyridin analogs20576327
fluoroquinolone-flavonoid hybridsAntimicrobial activity against Escherichia coli ATCC 35218, Bacillus subtilis ATCC 6633, Staphylococcus aureus ATCC 25923, Candida albicans ATCC 90873 and other drug resistant pathogensDesign, synthesis, and evaluation of novel fluoroquinolone-flavonoid hybrids as potent antibiotics against drug-resistant microorganisms.24769347
benzoxazinyl-oxazolidinones bearing nonaromatic heterocycle or aryl groupsMost active compound has MIC value of 0.25-0.5 ?g/mL against MRSADesign, synthesis, and structure-activity relationship studies of highly potent novel benzoxazinyl-oxazolidinone antibacterial agents.21955296
thioether pleuromutilin derivatives incorporating various heteroaromatic substituents into the C14 side chainMost potent derivates with MIC = 0.031-0.063 ?g/mLDesign, synthesis, and structure-activity relationship studies of novel thioether pleuromutilin derivatives as potent antibacterial agents.24874438
Ebsulfur derivatives (2-phenyl-1,2-benzisoselenazol-3(2H)-one (Ebselen) analogues with selenium replaced by sulfur)Potent activity against all S. aureus strains with MIC values mostly ?2?g/mLno mamalian cytotoxicityDevelopment of ebsulfur analogues as potent antibacterials against methicillin-resistant Staphylococcus aureus.27073054
4-chloro-flavanoneMICs of 30 ?g/mL in S. cerevesiae and 30 ?g/mL in C. neoformansDevelopment of non-natural flavanones as antimicrobial agents22039419
Diarylthiazole (DAT)bactericidal activity and active against drug-sensitive and resistant Mycobacterium tuberculosisDiarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.24967731
DifluoromethylornithineDFMO inhibited expression of the H. pylori virulence factor cytotoxin associated gene A, and its translocation and phosphorylation.Difluoromethylornithine is a novel inhibitor of Helicobacter pylori growth, CagA translocation, and interleukin-8 induction.21386987
(3S)-amino-(4R)-ethylpiperidinyl quinolonesactivity against resistant Staphylococcus aureus and Streptococcus pneumoniaeDiscovery of (3S)-amino-(4R)-ethylpiperidinyl quinolones as potent antibacterial agents with a broad spectrum of activity and activity against resistant pathogens.12904069
4-pyridone derivativesTwo 4-pyridone compounds exhibited strong antibacterial activities against 30 clinical isolates of methicillin-resistant S. aureus (MRSA) with MIC(90) of 0.5 and 2 mug/ml, respectively.Discovery of 4-Pyridone derivatives as specific inhibitors of enoyl-acyl carrier protein reductase (FabI) with antibacterial activity against Staphylococcus aureus.17420562
[(E)-N-methyl-N-(2-methyl-1H-indol-3-ylmethyl)-3-(7-oxo-5,6,7,8-tetrahydro-1,8-na phthyridin-3-yl)acrylamide]exquisite antistaphylococci activity, with 500 times lower MIC90 than currently available antibioticsDiscovery of a novel and potent class of FabI-directed antibacterial agents12234833
Phomallenic acid C (3)MIC of 3.9 microg/mL against wild-type S. aureus. superior to cerulenin and thiolactomycin, two most common FabF inhibitors.NADiscovery of bacterial fatty acid synthase inhibitors from a Phoma species as antimicrobial agents using a new antisense-based strategy. Fatty acids are essential for bacterial growth and viability, with the type II fatty acid synthesis (FAS II) pathway being a potential antibacterial target.16562839
kibdelomycinbacterial type II topoisomerase inhibitor, preferentially inhibiting the ATPase activity of DNA gyrase and topoisomerase IVDiscovery of kibdelomycin, a potent new class of bacterial type II topoisomerase inhibitor by chemical-genetic profiling in Staphylococcus aureus. Bacterial resistance to known therapeutics has led to an urgent need for new chemical classes of antibacterial agents.21867911
salicylidene acylhydrazide sulfonamidesromising activity at 50 ?M concentration against C. trachomatis and C. pneumoniae in HeLa cellsDiscovery of new polypharmacological antibacterial agents with multiple modes of actions can be an alternative to combination therapy and also a possibility to slow development of antibiotic resistance. New antichlamydial agents that also inhibit T3S (type III secretion) in Yersinia pseudotuberculosis.26204507
1-(3-bromo-2,3-dideoxy-2-fluoro-?-d-arabinofuranosyl)-5-ethyluracil (13) and 1-(?-d-arabinofuranosyl)-4-thio-5-hydroxymethyluracil (21) ,Compound 21 inhibited Mtb (H37Ra) (MIC(50)=0.5 ?g/mL) and M. bovis (MIC(50)=0.5 ?g/mL) at low concentrationsNo cellular toxicity of 13 or 21 was observed up to the highest concentration tested (CC(50)>100 ?g/mL)Discovery of novel 5-(ethyl or hydroxymethyl) analogs of 2'-'up' fluoro (or hydroxyl) pyrimidine nucleosides as a new class of Mycobacterium tuberculosis, Mycobacterium bovis and Mycobacterium avium inhibitors22664188
pyrazolopyridone analoguesin vitro bactericidal activity , a 4 log reduction in colony forming unitsDiscovery of pyrazolopyridones as a novel class of noncovalent DprE1 inhibitor with potent anti-mycobacterial activity.24818517
dithiazole thioneA novel non-toxic, non-haemolytic dithiazole thione derivative (DTT10) was identified as a potent competitive inhibitor of NorA efflux pump in S. aureus using in silico, in vitro and in vivo studies.Dithiazole thione derivative as competitive NorA efflux pump inhibitor to curtail multi drug resistant clinical isolate of MRSA in a zebrafish infection model. Lowrence Multi drug resistant (MDR) pathogens pose a serious threat to public health since they can easily render most potent drugs ineffective.27531512
dithiolopyrrolonesene-dithiol group of DTPs enables high-affinity metal binding as a central mechanism to inhibit metabolic processesDithiolopyrrolones (DTPs) are an underexplored class of disulfide-containing natural products, which exhibit potent antimicrobial activities against multidrug-resistant pathogens.28209778
DQ-113, quinoloneDQ-113 against: ofloxacin-resistant and methicillin-resistant S. aureus, MIC90 of 0.25microg/ml, all strains of Streptococcus pneumoniae, including penicillin-resistant strains, and Streptococcus pyogenes at 0.06 microg/ml, Enterococcus faecalis and Enterococcus faecium with MIC90s of 0.25 and 2 microg/ml, respectively, vancomycin-resistant enterococci, MIC range from 0.25 to 2 microg/ml, Haemophilus influenzae, including ampicillin-resistant strains (MIC90, 0.015 microg/ml), and Moraxella catarrhalis (MIC90, 0.03 microg/ml).DQ-113 also showed a potent activity against Haemophilus influenzae, including ampicillin-resistant strains (MIC90, 0.015 microg/ml), and Moraxella catarrhalis (MIC90, 0.03 microg/ml).11850285
DU-6859a, a new fluoroquinolone50% inhibitory concentrations of DU-6859a were 0.86 and 1.05 micrograms/ml for the supercoiling activities of DNA gyrases isolated from E. coli and P. aeruginosaDU-6859a showed potent broad-spectrum activity against gram-positive, gram-negative, and anaerobic bacteria, and its activity was greater than those of the control quinolones.8593031
VRT-125853 and VRT-752586, novel aminobenzimidazoleinhibit the essential ATPase activities of bacterial DNA gyrase and topoisomerase IVDual targeting of GyrB and ParE by a novel aminobenzimidazole class of antibacterial compounds.17116675
DX-619, a novel Des-F (6)-quinoloneThe MIC(90)s were: ?0.016 mg/L and 0.125 mg/L against methicillin-sensitive and -resistant S. aureus, 0.062 and 0.125 mg/L against methicillin-sensitive and -resistant S. epidermidis, respectively. The MIC(90)s for other bacteria are: penicillin-sensitive (0.016 mg/L) and -non-sensitive Streptococcus pneumoniae (0.062 mgL), Enterococcus faecalis (0.25 mg/L) and Enterococcus faecium (0.5 mg/L), Enterobacteriaceae (except for Escherichia coli) and glucose-nonfermenting bacilli (< or =4 mg/L)DX-619 was a potent antibacterial compound against multi-drug resistant bacteria including Gram-positive cocci, such as S. aureus and enterococci, which may warrant further exploration.18230543
Ebselen, an organoselenium clinical moleculeThe minimum inhibitory concentrations of ebselen at which 90% of clinical isolates of Enterococcus and Staphylococcus were inhibited (MIC90) were found to be 0.5 and 0.25 mg/L, respectively.Ebselen, an organoselenium clinical molecule, possesses potent antimicrobial activity against clinical multidrug-resistant Gram-positive pathogens, including Staphylococcus, Streptococcus, and Enterococcus, but not against Gram-negative pathogens.26222252
vanillin, ethyl vanillin, and vanillic acidMICs are 2 mg/ml ethyl vanillin, 3 mg/ml vanillin, and >8 mg/ml vanillic acid.Effect of vanillin, ethyl vanillin, and vanillic acid on the growth and heat resistance of Cronobacter species. Preservatives could be part of an effective intervention strategy for the control of Cronobacter species in foods, but few compounds with the desired antimicrobial properties have been identified to date.22186046
4''-Deoxy-4''-episubstituted arbekacin derivatives and 4''-epi-5-deoxy-5-episubstituted arbekacin derivatives5,4''-diepiarbekacin has more potency against Gram-positive and Gram-negative bacteria, 6'-N-methyl derivative of the 5,4''-diepiarbekacin was effective against P. aeruginosaEffect of varying the 4''-position of arbekacin derivatives on antibacterial activity against MRSA and Pseudomonas aeruginosa.17889537
Biphenyl derivativeFtsZ inhibitor (Kd = 0.5 ?M) with high antibacterial activity [MIC (MRSA) = 7 ?MEffective GTP-replacing FtsZ inhibitors and antibacterial mechanism of action25486266
bis-naphthoquinone thiol-crown ether 7aActive against Staphylococcus aureus methicillin resistance with MIC value of 2.68 microMEfficient synthesis of 'redox-switched' naphthoquinone thiol-crown ethers and their biological activity evaluation11937353
Sugar (Man, Fuc, and Gal)BALB/c mice (male; 6?8 wk old; Taconic Farms) were anesthetized with Avertin [250 mg/kg intraperitoneally (IP)], and 50 ?l of 2 ? 108 PAO1 or PDO300 in PBS or PBS containing sugars (5 mM Man+5 mM Fuc+5 mM Gal or 15 mM Fuc) were intratracheally instilled into the lung by a feeding needle (24 gauge)Our findings reveal that sugar inhalation, an inexpensive and safe therapeutic, could be used in combination with conventional antibiotic therapy to more effectively treat P. aeruginosa lung infections.Epub 2013 Jun 21. Sugar administration is an effective adjunctive therapy in the treatment of Pseudomonas aeruginosa pneumonia. Treatment of acute and chronic pulmonary infections caused by opportunistic pathogen Pseudomonas aeruginosa is limited by the increasing frequency of multidrug bacterial resistance.23792737
21-((1H-imidazol-5-yl)methyl)-pseudopteroxazole (7a)Activity against both replicating and non-replicating persistent forms of M.tuberculosisnear absence of in vitro cytotoxicityEvaluation of pseudopteroxazole and pseudopterosin derivatives against Mycobacterium tuberculosis and other pathogen23015770
SCA-50Potent concentration-dependent bactericidal activity against MRSA Mu50 strain and very importantly, 2-60 fold more potent inhibitory effect on MRSA Mu50 than all the commonly used antibioticsEvaluation of small molecule SecA inhibitors against methicillin-resistant Staphylococcus aureus26432604
triazol-1-yl-pyrimidines (AVS2087, AVS2093, AVS2387, and AVS2236)AVS2087, AVS2093, AVS2387, and AVS2236, were identified as potent inhibitors of catalytic subunit with IC(50) values of 1.0 +/- 0.02, 1.0 +/- 0.04, 2.1 +/- 0.12, and 2.0 +/- 0.08 microM, respectivelyEvaluation of substituted triazol-1-yl-pyrimidines as inhibitors of Bacillus anthracis acetohydroxyacid synthase20170757
T-3811ME (BMS-284756), a new des-F(6)-quinoloneT-3811, the free base of T-3811ME, exhibited potent activity against 28 clinical strains of PRSP at MIC90 0.0625 microg/mlEvaluation of T-3811ME (BMS-284756), a new des-F(6)-quinolone, for treatment of meningitis caused by penicillin-resistant Streptococcus pneumoniae in rabbits12019087
2-phenyl-4(1H)-quinolone and 2-phenyl-4-hydroxyquinoline derivativesThe 2-phenyl-4-hydroxyquinoline derivatives 28f and 29f display potent EPI activity against SA-1199BEvolution from a natural flavones nucleus to obtain 2-(4-Propoxyphenyl)quinoline derivatives as potent inhibitors of the S. aureus NorA efflux pump21751791
Farnesol300 ?M of farnesol or vancomycin: 40 mg/L and rifampicin: 10 mg/LNAFarnesol, a quorum-sensing molecule in Candida albicans, has been described as impairing growth of several different microorganisms and we have previously shown its potential as an adjuvant in antimicrobial therapy against S. epidermidis. Farnesol might induce biofilm detachment, as determined by the reduced biofilm biomass, which can partially explain the previous findings regarding its role as a possible chemotherapy adjuvant.22591918
d-lysine conjugated tetradecanoyl analogue (D-LANA-14)anti-MRSA activity (MIC = 3.1-6.3 ?g/mL)No skin toxicity even at high concentrationFatty Acid Comprising Lysine Conjugates: Anti-MRSA Agents That Display In Vivo Efficacy by Disrupting Biofilms with No Resistance Development28225264
1,4-benzothiazine derivativesAlmost all derivatives evaluated showed good activity in combination with ciprofloxacin against S. aureus ATCC 25923; some were capable of completely restoring ciprofloxacin activity in a norA-overexpressing strain (SA-K2378)From phenothiazine to 3-phenyl-1,4-benzothiazine derivatives as inhibitors of the Staphylococcus aureus NorA multidrug efflux pump18578473
sulfonamide derivatives of the alpha-(R)-amino hydroxamic acids, (BB-78484 and BB-78485)antibacterial activities against Escherichia coliFrom this screen, a series of sulfonamide derivatives of the alpha-(R)-amino hydroxamic acids, exemplified by BB-78484 and BB-78485, have been identified as having potent inhibitory activities against LpxC in an in vitro assay.12019092
naphtho-?-pyrones (fonsecinones A and C and aurasperones A and E)Fonsecinone A exhibited the most potent antibacterial activity, with minimum inhibitory concentrations (MICs) of 4.26, 17.04, and 4.26 ?g/mL against ESBL-producing E. coli, P. aeruginosa, and E. faecalis, respectively.Fungal naphtho-?-pyrones: Potent antibiotics for drug-resistant microbial pathogens27063778
Histidine (His) derived lipo-amino acids having pendant lipid tails at N(?)- and N(?)-positions on imidazole group of Hisantimicrobial activity against Gram-positive and Gram-negative bacteria, also strong anti-MRSA activityFurthermore, our designed His-derived lipo-peptidomimetics (HDLPs) consisting of two or three residues displayed strong anti-MRSA activity and protease stability as well as retained potent antimicrobial activity under high salt concentration.23933046
biricodar (VX-710) and timcodar (VX-853)lowers MICs of several clinically used antibioticsFurthermore, these compounds were effective in lowering the MICs of several clinically used antibiotics, including fluoroquinolones, suggesting that VX-710 and VX-853 are representatives of a new class of bacterial efflux inhibitors with the potential for use in combination therapy.15504837
Gallium Compounds ( Ga-protoporphyrin, Ga(NO3)3 and other Ga compounds)Activity against Mycobacterium abscessus, Ga-protoporphyrin was >20 times more active than Ga(NO3)3Gallium Compounds Exhibit Potential as New Therapeutic Agents against Mycobacterium abscessus26033732
GE23077Selective inhibitor of bacterial RNA polymerase (RNAP), It inhibits Gram-positive (Bacillus subtilis) and Gram-negative (Escherichia coli) RNAPs with IC50 values in the 10(-8) m rangeGE23077, a novel microbial metabolite recently isolated from Actinomadura sp. culture media, is a potent and selective inhibitor of bacterial RNA polymerase (RNAP).15265034
GSK1322322GSK1322322 had an MIC(90) of 1 ?g/ml against M. catarrhalis and 4 ?g/ml against H. influenzae, with 88.8% of ?-lactamase-positive strains showing growth inhibition at that concentration. All S. pneumoniae strains were inhibited by ? 4 ?g/ml of GSK1322322, with an MIC(90) of 2 ?g/ml.Given the antibacterial potency demonstrated against this panel of organisms, GSK1322322 represents a valuable alternative therapy for the treatment of infectious diseases caused by drug-resistant pathogens.23478958
Green-leaf-derived C6-aroma compoundsThe most effective compound was (3E)-hexenal at concentrations of 0.1 and 1 microg mL(-1), which killed 2.1 x 10(5) cfu mL(-1) of S. aureus IFO 12732 and 1.4 x 10(5) cfu mL(-1) of E. coli IFO 3301Green-leaf-derived C6-aroma compounds with potent antibacterial action that act on both Gram-negative and Gram-positive bacteria.12475283
1-beta-D-2'-arabinofuranosyl and 1-(2'-deoxy-2'-fluoro-beta-D-ribofuranosyl) pyrimidine nucleosides possessing diverse sets of alkynyl, alkenyl, alkyl, and halo substituents at the C-5 position of the uracilActivity against M. tuberculosis, M. bovis, and M. avium with MIC similar or close to that of the reference drug rifampicinGrowth inhibition of Mycobacterium bovis, Mycobacterium tuberculosis and Mycobacterium avium in vitro: effect of 1-beta-D-2'-arabinofuranosyl and 1-(2'-deoxy-2'-fluoro-beta-D-2'-ribofuranosyl) pyrimidine nucleoside analogs17602465
sulfonyl piperazine and pyrazole compoundsHere we describe the discovery and characterization of sulfonyl piperazine and pyrazole compounds, each with novel mechanisms of action. E. coli mutants resistant to these compounds display no cross-resistance to antibiotics of other classes.25733621
7-Cl and 7-CF3 substituted N-dodecylamino-4-aminoquinolines (5 and 10)biofilm formation inhibitors with 50% biofilm inhibition at 69 ?M and 63 ?M in S. marcescens and P. aeruginosaHere we report a new type of highly potent 4-aminoquinoline derivatives as quorum sensing inhibitors in Serratia marcescens and Pseudomonas aeruginosa, exhibiting weak bactericidal activities (minimum inhibitory concentration (MIC) > 400 ?M).28350449
1-Hydroxypyridine-2(1H)-thione-6-carboxylic AcidInhibition Ki 13 nm against VIM-2 (carbapenem-hydrolyzing metallo ?-lactamases (MBL)) that corresponds to a remarkable 0.99 ligand efficiency.low cytotoxicity (CC50 ) of 97 ?m with a corresponding therapeutic index of 880Here we report the discovery of 1-hydroxypyridine-2(1H)-thione-6-carboxylic acid (3) as a first-in-class metallo ?-lactamase inhibitor (MBLi) with a potent inhibition Ki of 13 nm against VIM-2 that corresponds to a remarkable 0.99 ligand efficiency.28482143
Hydantoin (imidazolidinedione) derivativesbactericidal and also prevent the development of methicillin-resistant Staphylococcus aureus (MRSA) bacterial resistanceHerein, we report the design of bacterial membrane-active hydantoin derivatives, from which we identified compounds that show much more potent antimicrobial activity than nitrofurantoin against a panel of clinically relevant Gram-positive and Gram-negative bacterial strains.28984451
purine benzimidazole hybridsThe most potent analogue has MIC = 4 ?g/mL against multidrug-resistant strains Staphylococcus aureusHexyl appended hybrid 3c gave potent activities against most of the tested bacteria and fungi especially against multidrug-resistant strains Staphylococcus aureus (MIC = 4 ?g/mL).29598912
taurine haloamines (TauCl and TauBr)However, a combined therapy, an application of TauBr together with other anti-biofilm agents (e.g., DNase), seems to be more promising. DOI: 10.1007/978-1-4614-6130-2_2323392942
beta-sulfonyl- and beta-sulfinylhydroxamic acid derivativespotent inhibitors of Escherichia coli peptide deformylase (PDF)., antibacterial activities against Chlamydia pneumoniae, Mycoplasma pneumoniae, Haemophilus influenzae, and Moraxella catarrhalis.Hydroxamic acid derivatives as potent peptide deformylase inhibitors and antibacterial agents.10882358
1-benzyl-3-cetyl-2-methylimidazolium iodide, NH125Active against oxacillin-resistant Staphylococcus aureus (ORSA), vancomycin-resistant Enterococcus faecalis (VRE), penicillin-resistant Streptococcus pneumoniae (PRS)Identification and characterization of a potent antibacterial agent, NH125 against drug-resistant bacteria. New imidazole compounds were synthesized to develop a novel and effective antibacterial agent (1-benzyl-3-cetyl-2-methylimidazolium iodide, NH125).10830522
ABTZ-1, benzothiazolium salt,Potent activity against multidrug-resistant clinical isolates of methicillin-resistant S. aureus (MRSA) and vancomycin-resistant enterococci (VRE)low hemolytic activityIdentification of a novel protein synthesis inhibitor active against gram-positive bacteria22362659
AminoPYrimidine-Sulfonamide (APYS1)bactericidal activity against M. tuberculosisIdentification of aminopyrimidine-sulfonamides as potent modulators of Wag31-mediated cell elongation in mycobacteria.27677649
novel series of quinoxaline 1,4-di-N-oxidesIn general, all compounds were active with ratios of MICs against resistant and non-resistant strains of If the bactericidal activity and activity on non-replicating bacteria in vitro translate to in vivo conditions, quinoxaline 1,4-di-N-oxides may offer a path to shortened therapy. DOI: 10.1093/jac/dkn214 PMCID: PMC257495918502817
a biomimetic iron-sequestering polymer (PAI-DHBA)NAIn addition, bacterial growth was more susceptible to antibiotics combined with PAI-DHBA. Multivalent polymers that bind and sequester iron, such as PAI-DHBA, offer a promising early intervention or adjuvant to antibiotics.25872681
BC-3781 is a novel semisynthetic pleuromutilin antibioticBC-3781 against: ABSSSI such as Staphylococcus aureus (MIC50/90, 0.12/0.12 ?g/ml; 99.8% inhibited at ?0.5 ?g/ml), beta-hemolytic streptococci (MIC50/90, 0.03/0.03 ?g/ml; 99.3% inhibited at ?0.5 ?g/ml), and coagulase-negative staphylococci (CoNS; MIC50/90, 0.06/0.12 ?g/ml; 97.8% inhibited at ?1 ?g/ml), also methicillin-susceptible (MSSA) and methicillin-resistant (MRSA) S. aureus strains. against Enterococcus faecium, with 76.3% of vancomycin-susceptible and 97.0% of vancomycin-resistant isolates at ?1 ?g/ml. Beta-hemolytic and viridans group streptococci 99.3% and 96.7% of isolates inhibited at ?0.5 ?g/ml, respectively, Streptococcus pneumoniae (MIC50/90, 0.12/0.25 ?g/ml), Haemophilus influenzae (MIC50/90, 1/2 ?g/ml), and Moraxella catarrhalis (MIC50/90, 0.12/0.25 ?g/ml) no negative influence by ?-lactamase or resistance to other antimicrobial classes tested.In all, BC-3781 displayed a very potent antibacterial profile including the most prevalent bacterial pathogens causing ABSSSI and CABP, thus warranting further clinical development of this antibiotic in these and possibly other indications.23836172
DS-8587, novel fluoroquinoloneMore effective antibacterial activity when compared with ciprofloxacin and levofloxacin.In conclusion, DS-8587 exhibits potent antibacterial activity against quinolone-resistant A. baumannii isolates that harbor mutations in quinolone resistance-determining regions.24709045
polymyxin B and SERMsSynergistic killing against the polymyxin-resistant P. aeruginosa, K. pneumoniae, and A. baumannii isolates as demonstrated by a ?2-3 log10 decrease in bacterial count (CFU/ml) after 24 hours.In conclusion, the combination of polymyxin B and SERMs illustrated a synergistic activity against XDR Gram-negative pathogens, including highly polymyxin-resistant P. aeruginosa isolates, and represents a novel combination therapy strategy for the treatment of infections because of problematic XDR Gram-negative pathogens. DOI: 10.1089/mdr.2016.019627935770
WQ-3810, a new fluoroquinoloneAgainst A. baumannii, including MDR isolates, MIC(90))=1 mg/L, against E. coli and S. pneumoniae, including FQR isolates, MIC(90)=4 mg/L and 0.06 mg/L, respectivelyIn conclusion, this study demonstrated that WQ-3810 exhibits extremely potent antibacterial activity over the existing fluoroquinolones, particularly against MDR and FQR pathogens.25239276
TAM16TAM16 has excellent pharmacological and safety profiles, and the frequency of resistance for TAM16 is ?100-fold lower than INHIn multiple mouse models of TB infection, TAM16 showed in vivo efficacy equal to the first-line TB drug isoniazid, both as a monotherapy and in combination therapy with rifampicin.28669536
3,4-Dihydropyrimidinone-coumarin analoguesMIC values against the drug susceptive S. aureus ranging from 0.2 to 6.25?g/mLIn search of potent antibiotic, taking coumarin and dihydropyrimidinone as lead compound, a green, eco-friendly and efficient protocol has been developed and synthesized the dihydropyrimidin-2(1H)-one/thione derivatives of coumarin 3/4 from substituted 4-formylcoumarins 2 and ethylacetoacetate using urea/thiourea in the presence of catalytic amount of ceric ammonium nitrate is reported.28094219
BAS-118, a new benzamide derivativeMIC(50), MIC(90) and MIC range of BAS-118 for 100 randomly selected isolates of H. pylori were In summary, BAS-118 is a novel anti-H. pylori agent with a potent and selective antibacterial activity, which includes CAM- and MNDZ-resistant isolates.12096019
Battacin or octapeptin B5MICs of 2 to 4 ?g/ml against hospital strains of Escherichia coli and Pseudomonas aeruginosaIn the current study, we report the isolation, structure elucidation, and preliminary biological characterization of a new cationic lipopeptide antibiotic, battacin or octapeptin B5, produced from a Paenibacillus tianmuensis soil isolate22183171
PLEX (biodegradable Polymer-Lipid Encapsulation MatriX)-doxycycline coating on titanium alloy implantsthe PLEX-doxycycline coating on titanium alloy implants provided complete protection against implant-associated MSSA osteomyelitis, and resulted in a significant reduction in the number of culture positive samples when challenged with a doxycycline-resistant MRSA.NAIn the present study, we investigated the efficacy of a biodegradable Polymer-Lipid Encapsulation MatriX (PLEX) loaded with the antibiotic doxycycline as a local prophylactic strategy against implant-associated osteomyelitis.25910578
complestatin abd related compounds (neuroprotectin A and chloropeptin I )Inhibited S. aureus FabI with IC?? of 0.3-0.6 ?M, prevented the growth of S. aureus as well as methicillin-resistance S. aureus (MRSA) and quinolone-resistant S. aureus (QRSA), with minimum inhibitory concentrations (MICs) of 2-4 ?g/mL.In the screening of inhibitors of Staphylococcus aureus enoyl-ACP reductase (FabI), complestatin was isolated as a potent inhibitor of S. aureus FabI together with neuroprotectin A and chloropeptin I from Streptomyces chartreusis AN1542.25947917
8T-W, a novel synthetic dienoyl tetramic acidantimicrobial activity against Gram-positive and Gram-negative anaerobes as well as staphylococciIn this paper, we report on a novel series of synthetic dienoyl tetramic acids that lack a complex dioxabicyclononane unit. Several of these compounds, particularly 8T-W, exhibit potent antimicrobial activity against Gram-positive and Gram-negative anaerobes as well as staphylococci.2709374
pyrrolo[1,5-a]pyrazine-based analoguesMost significantly, by in vitro Mtb culture assays, we confirmed that our Eis (Enhanced Intracellular Survival) inhibitors were capable of penetrating the Mtb cell wall and canceling the KAN resistance of Mtb K204, which overexpresses Eis. IC50 (microM) 0.039 - 8.7 against purified Eis_Mtb enzyme. MIC of KAN against Mtb H37Rv in the presence of these compounds <= 1.25 micrograms/mL, MIC of KAN against Mtb K204 range 1.25 micrograms/mL to > 10 micrograms/mLIn this paper, we report the discovery and development of pyrrolo[1,5-a]pyrazine-based analogues as highly potent inhibitors of the Mycobacterium tuberculosis (Mtb) acetyltransferase enhanced intracellular survival (Eis), whose up-regulation causes clinically observed resistance to the aminoglycoside (AG) antibiotic kanamycin A (KAN).28192916
1-substituted-5-[(3,5-dinitrobenzyl)sulfanyl]-1H-tetrazoles and their oxa and selanyl analogs(MIC) values reached 1 ?M (0.36-0.44 ?g/mL) against Mycobacterium tuberculosis CNCTC My 331/88 and 0.25-1 ?M against six multidrug-resistant clinically isolated strains of M. tuberculosis.In this work, a new class of highly potent antituberculosis agents, 1-substituted-5-[(3,5-dinitrobenzyl)sulfanyl]-1H-tetrazoles and their oxa and selanyl analogs, is described.24927053
trans-3,5-disubstituted pyrrolidinylthio-1beta-methylcarbapenemspotent activities against methicillin-resistant Staphylococcus aureus and Pseudomonas aeruginosaIn vitro activities of novel trans-3,5-disubstituted pyrrolidinylthio-1beta-methylcarbapenems with potent activities against methicillin-resistant Staphylococcus aureus and Pseudomonas aeruginosa.10681308
E-1040 [(6R,7R)-3-[(4-carbamoyl-1-quinuclidinio)methyl]-7-[2-(5-amino-1,2 ,4- thiadiazol-3-yl)-(Z)-2-methoxyiminoacetoamido]-8-oxo-5-thia- 1- azabicyclo(4,2,0)oct-2-ene-2-carboxylate]MIC50 ?0.25 microgram/ml and the MIC90 0.06 to 2 micrograms/ml against Enterobacteriaceae, Pseudomonas aeruginosa, and Haemophilus and NeisseriaIn vitro activity of E-1040, a novel cephalosporin with potent activity against Pseudomonas aeruginosa. The in vitro activity of E-1040 [(6R,7R)-3-[(4-carbamoyl-1-quinuclidinio)methyl]-7-[2-(5-amino-1,2 ,4- thiadiazol-3-yl)-(Z)-2-methoxyiminoacetoamido]-8-oxo-5-thia- 1- azabicyclo(4,2,0)oct-2-ene-2-carboxylate], a novel cephalosporin, was compared with that of ceftazidime, cefpirome, cefepime, imipenem, and gentamicin.3150915
2-(thiazol-2-ylthio)-1beta-methylcarbapenems (SM-197436, SM-232721, and SM-232724)MIC(90) of In vitro and in vivo activities of novel 2-(thiazol-2-ylthio)-1beta-methylcarbapenems with potent activities against multiresistant gram-positive bacteria.12878507
PD 0305970 and PD 0326448 (quinazoline-2,4-diones)MIC90 ranges were: staphylococci (0.125 to 0.5 ?g/ml), streptococci (0.03 to 0.06 ?g/ml) , enterococci (0.25 to 2 ?g/ml) and 0.25 to 0.5 ?g/ml for Moraxella catarrhalis, Haemophilus influenzae, Listeria monocytogenes, Legionella pneumophila, and Neisseria sppIn vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.17261623
RBx 14255, KetolideThe MIC(90) Clostridium difficile was 4 ?g/ml (MIC range, 0.125 to 8 ?g/ml)In vitro and in vivo activities of the novel Ketolide RBx 14255 against Clostridium difficile22869573
CS-023 (RO4908463), 1beta-methylcarbapenem with 5-substituted pyrrolidin-3-ylthio groups, including an amidine moiety at the C-2 positionMost potent activity against P. aeruginosa and MRSA, with MIC90s of 4 microg/ml and 8 microg/ml, respectively.In vitro and in vivo antibacterial activities of CS-023 (RO4908463), a novel parenteral carbapenem16048932
ER-35786Active against methicillin-susceptible Staphylococcus aureus and streptococci (MIC90S < or = 0.39 ?g/ml), methicillin-resistant S. aureus(MIC90 12.5 ?g/ml), Enterobacteriaceae, Moraxella catarrhalis, and Haemophilus influenzae (MIC90 < or = 1.56?g/ml)In vitro and in vivo antibacterial activities of ER-35786, a new antipseudomonal carbapenem. ER-35786 is a new parenteral 1 beta-methyl carbapenem with a broad antibacterial spectrum and a potent antipseudomonal activity.9021183
AM-833, a new quinolone derivativepotent activity against members of the family Enterobacteriaceae, Neisseria spp., and Haemophilus influenzae and good activity against staphylococci, Pseudomonas aeruginosa, and Branhamella catarrhalisIn vitro and in vivo antibacterial activity of AM-833, a new quinolone derivative. AM-833 showed potent activity against members of the family Enterobacteriaceae, Neisseria spp., and Haemophilus influenzae and good activity against staphylococci, Pseudomonas aeruginosa, and Branhamella catarrhalis.2942103
gallium nitrate Ga(NO(3))(3)inhibits the growth of a collection of 58 A. baumannii strains in both chemically defined medium and human serum, at concentrations ranging from 2 to 80 ?M and from 4 to 64 ?M, respectively.In vitro and in vivo antimicrobial activities of gallium nitrate against multidrug-resistant Acinetobacter baumannii. Multidrug-resistant Acinetobacter baumannii poses a tremendous challenge to traditional antibiotic therapy.22964249
A-80556, new fluoroquinoloneMIC90 values: Staphylococcus aureus (0.12 ?h/ml), Streptococcus pneumoniae (0.12 ?h/ml), Escherichia coli (0.06 ?h/ml), Pseudomonas aeruginosa ( 4.0 ?h/ml), Bacteroides fragilis ( 2.0 ?h/ml)In vitro and in vivo evaluations of A-80556, a new fluoroquinolone. A-80556 is a novel fluoroquinolone with potent antibacterial activity against gram-positive, gram-negative, and anaerobic organisms.8067740
S-013420, a novel bicyclolideMost potent activity against erythromycin-intermediate and -resistant S. pneumoniae with an MIC(90) of 0.25 mg/L and inhibited the growth of all strains of S. pyogenes with macrolide resistance genes at 1 mg/L, MIC(90) values of 0.125, 0.125, 8 and 0.5 mg/L for Streptococcus pneumoniae, Streptococcus pyogenes, Haemophilus influenzae and Moraxella catarrhalis, respectivelyIn vitro antibacterial activities of S-013420, a novel bicyclolide, against respiratory tract pathogens20472695
AZD0914, a new spiropyrimidinetrioneBacterial DNA gyrase/topoisomerase inhibitor with potent in vitro antibacterial activity against Gram-positive (Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pneumoniae, Streptococcus pyogenes, and Streptococcus agalactiae), fastidious Gram-negative (Haemophilus influenzae and Neisseria gonorrhoeae), atypical (Legionella pneumophila), and anaerobic (Clostridium difficile) bacterial speciesIn vitro antibacterial activity of AZD0914, a new spiropyrimidinetrione DNA gyrase/topoisomerase inhibitor with potent activity against Gram-positive, fastidious Gram-Negative, and atypical bacteria.25385112
BMY-28142most potent against Enterobacteriaceae with a MIC90 0.12 micrograms/mlIn vitro antibacterial activity of BMY-28142, a new extended-spectrum cephalosporin.3859244
SM-7338, a new carbapenem antibioticAt a concentration of 0.5 micrograms/ml, SM-7338 inhibited 90% of these strains: Staphylococcus aureus, beta-hemolytic streptococci, Streptococcus pneumoniae, Haemophilus influenzae, Neisseria spp., members of the family Enterobacteriaceae, Pseudomonas spp., and gram-positive and gram-negative anaerobes.In vitro antibacterial activity of SM-7338, a carbapenem antibiotic with stability to dehydropeptidase I. SM-7338, a new carbapenem antibiotic, was demonstrated to have potent antibacterial activity against a broad spectrum of aerobes, including Staphylococcus aureus, beta-hemolytic streptococci, Streptococcus pneumoniae, Haemophilus influenzae, Neisseria spp., members of the family Enterobacteriaceae, Pseudomonas spp., and gram-positive and gram-negative anaerobes in a collection of 1,102 unselected clinical isolates.2655530
ABT-492, new fluoroquinoloneActivity against Enterobacteriaceae, gram-negative species including Haemophilus influenzae, Moraxella catarrhalis, Neisseria gonorrhoeae, Legionella spp. , Pseudomonas aeruginosa and Helicobacter pylori.In vitro antibacterial potency and spectrum of ABT-492, a new fluoroquinolone. ABT-492 demonstrated potent antibacterial activity against most quinolone-susceptible pathogens.14506039
AT-2266, new pyridonecarboxylic acidinhibited some gram-positive bacteria, such as staphylococci and Bacillus subtilis, and most gram-negative bacteria, including Serratia marcescens, Pseudomonas aeruginosa, Haemophilus influenzae, and Campylobacter jejuni, at concentrations of 0.1 to 0.78 microgram/ml, and most gram-positive bacteria, glucose-nonfermenters, and Mycoplasma pneumoniae at concentrations of 1.56 to 12.5 micrograms/ml.:In vitro antibacterial properties of AT-2266, a new pyridonecarboxylic acid. AT-2266, 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-1,8-naphthyridine-3 -carboxylic acid, is a new pyridonecarboxylic acid derivative with broad and potent antibacterial activity.6575721
ACH-702, a novel isothiazoloquinolonein vitro antibacterial activity against Mycobacterium tuberculosis, with MICs of In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.20516287
ABT-492, a novel quinolonepenicillin-sensitive, resistant, and levofloxacin-resistant Streptococcus pneumoniae strains : MICs 0.0078 to 0.125 micro g/ml; beta-lactamase-positive and beta-lactamase-negative Haemophilus influenzae strains: MICs 0.000313 to 0.00125 micro g/ml; beta-lactamase-positive and beta-lactamase-negative Moraxella catarrhalis strains : MICs 0.001 to 0.0025 micro g/mlIn vitro pharmacodynamic activities of ABT-492, a novel quinolone, compared to those of levofloxacin against Streptococcus pneumoniae, Haemophilus influenzae, and Moraxella catarrhalis.14693540
ABI-0043, novel rifamycinBactericidal activity against clinical isolates of methicillin-resistant Staphylococcus aureus (MRSA) and methicillin-susceptible S. aureus (MSSA)In vitro pharmacodynamics of novel rifamycin ABI-0043 against Staphylococcus aureus.18400804
DQ-113, new quinoloneActivity against against Streptococcus pneumoniaeIn vivo efficacy of a new quinolone, DQ-113, against Streptococcus pneumoniae in a mouse model. DQ-113 is a new quinolone with potent activity against gram-positive pathogens.14638468
NITD-304 and NITD-349potent activity against both drug-sensitive and multidrug-resistant clinical isolates of MtbIndolcarboxamide is a preclinical candidate for treating multidrug-resistant tuberculosis24307692
5-acetylenic derivatives of 2',3'-dideoxyuridine (3-8) and 3'-fluoro-2',3'-dideoxyuridine (22-27)2',3'-Dideoxyuridine possessing 5-decynyl, 5-dodecynyl, 5-tridecynyl, and 5-tetradecynyl substituents (4-7), 3'-fluoro-2',3'-dideoxyuridine derivative 5-tetradecynyl analogue (26), displayed the most potent activity against all mycobacteria. 2-amino-6-mercaptoethyl-9-(2,3-dideoxy-beta-d-glyceropentofuranosyl)purine (32) and 2-amino-4-fluoro-7-(2,3-dideoxy-beta-d-glyceropentofuranosyl)pyrrolo[2,3-d]pyrimidine (35) were the most efficacious against M. bovis and M. tuberculosis, and M. avium, respectivelyInhibition of Mycobacterium tuberculosis, Mycobacterium bovis, and Mycobacterium avium by novel dideoxy nucleosides17696514
JNJ-Q2, new fluoroquinolonein vitro activity against Gram-negative and Gram-positive organisms, including methicillin-resistant Staphylococcus aureus (MRSA) and ciprofloxacin-resistant MRSA isolates, with MICs ? 0.12 ?g/mInhibition of S. aureus DNA gyrase and DNA topoisomerase IV enzymes demonstrated that JNJ-Q2 was more potent than comparators against wild-type enzymes and enzymes carrying quinolone-resistant amino acid substitutions, and JNJ-Q2 displayed equipotent activity against both enzymes.21911562
1-(2-benzoxazolyl)-3,3,3-trifluoro-2-propanone (TF18), a trifluoromethyl ketone derivativeInhibitory activity against clarithromycin-susceptible and-resistant Helicobacter pyloriInhibitory action of a new proton pump inhibitor, trifluoromethyl ketone derivative, against the motility of clarithromycin-susceptible and-resistant Helicobacter pylori.15194136
chlorhexidine with trisEDTA or miconazoleChlorhexidine/miconazole MICs (median = 0.5 mg/L) were lower than those of either drug alone (P < 0.05) and lower than chlorhexidine/trisEDTA MICs (median = 1 mg/L; P < 0.0005) in each bacterial type and from both regions, except for miconazole in NUK MSSP.Interaction of chlorhexidine with trisEDTA or miconazole in vitro against canine meticillin-resistant and -susceptible Staphylococcus pseudintermedius isolates from two UK regions. Clark SM(1), Loeffler A(2), Schmidt VM(3), Chang YM(2), Wilson A(2), Timofte D(3), Bond R(2). Author information: (1)Department of Clinical Sciences and Services, Royal Veterinary College, Hawkshead Lane, North Mymms, Hatfield, Hertfordshire, AL9 7TA, UK. sclark@rvc.ac.uk. (2)Department of Clinical Sciences and Services, Royal Veterinary College, Hawkshead Lane, North Mymms, Hatfield, Hertfordshire, AL9 7TA, UK. (3)School of Veterinary Science, University of Liverpool, Chester High Road, Neston, CH64 7TE, UK. BACKGROUND: Topical therapy is an important alternative to systemic antibacterial therapy for treatment of canine superficial pyoderma in light of the emergence of multidrug-resistant staphylococci.27406860
Carbohydrate derived fulvic acid (CHD-FA)minimum inhibitory concentration of 0.5%.Despite the widespread use of mouthwashes being used as adjunctive measures to control these biofilms, their prolonged use is not recommended due to various side effects.Investigating the biological properties of carbohydrate derived fulvic acid (CHD-FA) as a potential novel therapy for the management of oral biofilm infections.24063298
diethyl malate and 1-methyl malatediethyl malate and 1-methyl malate can decrease the MIC value of benzyl penicillin by sixteen and eight-foldInvestigation for antimicrobial resistance-modulating activity of diethyl malate and 1-methyl malate against beta-lactamase class A from Bacillus licheniformis by molecular dynamics, in vitro and in vivo studies.24836845
lucensimycinsLucensimycin E (5) exhibited the best activity and showed MIC values of 32 microg/mL against Staphylococcus aureus and 8 microg/mL against Streptococcus pneumoniae.Isolation, structure, and antibacterial activities of lucensimycins D-G, discovered from Streptomyces lucensis MA7349 using an antisense strategy. Bacterial resistance to existing antibiotics continues to grow, necessitating the discovery of new compounds of this type.19115838
PC-904, sodium 6-{d(-)-alpha-(4-hydroxy-1,5-naphthyridine-3-carboxamido) phenylacetamido}-penicillanateAgainst systemic infections with P. aeruginosa, K. pneumoniae, and E. coli in mice, PC-904 is 7 to 10 times, over 8 times, and 2 to 15 times more active than carbenicillinIt is confirmed that PC-904 has a very potent in vivo antibacterial activity against gram-negative and gram-positive organisms.1046355
JNJ-Q2, a new fluoroquinoloneMIC(50) and MIC(90), 0.12 and 0.5 ?g/ml respectivelyJNJ-Q2, a new fluoroquinolone with potent in vitro activity against Staphylococcus aureus, including methicillin- and fluoroquinolone-resistant strains.21555765
Lactam hybrid analogues of solonamide B and autoinducing peptidesS. aureus AgrC antagonistsLactam hybrid analogues of solonamide B and autoinducing peptides as potent S. aureus AgrC antagonists.29738955
Undecatungsto(ferri)ferrosilicate ([SiW11O39Fe](6/5-))Lacunary-substituted undecatungstosilicates sensitize methicillin-resistant Staphylococcus aureus to beta-lactams.11558574
Laser-assisted nasal decolonization25 patients colonized with MSSA/MRSA were allocated to 4 treatment arms; low-power, dual-wavelength 870-/930-nm laser alone (GR1); low-power, dual-wavelength laser followed by erythromycin (E-mycin) cream (GR2); low-power, dual-wavelength laser followed by peroxide irrigation (GR3); and high-power 940-nm laser alone (GR4).No adverse events or discomfort were reported.Laser therapy can eradicate MRSA and potentially resensitization of bacteria to the antimicrobial effect of erythromycin. Nasal decolonization for GR1, GR2, GR3, and GR4 was 1 of 3, 13 of 14, 2 of 4, and 4 of 4, respectively22503099
LCB01-0648 OxazolidinonesMIC90s 0.5 mg/L against the methicillin-resistant Staphylococcus aureus (MRSA) and methicillin-resistant coagulase-negative staphylococci (MRCNS)LCB01-0648 showed the most potent antimicrobial activities against clinically isolated Gram-positive bacteria.28273820
Q203, an imidazo[1,2-a]pyridine amide derivativeactivity against Mycobacterium tuberculosis H37RvLead optimization of a novel series of imidazo[1,2-a]pyridine amides leading to a clinical candidate (Q203) as a multi- and extensively-drug-resistant anti-tuberculosis agent.24870926
lipo-?-AApeptidesPotent broad-spectrum activities against fungi and a series of Gram-positive and Gram-negative bacteriaLipo-?-AApeptides as a new class of potent and broad-spectrum antimicrobial agents.22475244
Marinomycin AMarinomycin A is a member of a new class of bis-salicylate-containing polyene macrodiolides, which have potent antibiotic activity against methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus faecium.22824902
(?)-marinopyrrole A and its derivativespara-trifluoromethyl analog (33) of marinopyrrole A is ? 63-, 8-, and 4-fold more potent than vancomycin against methicillin-resistant Staphylococcus epidermidis (MRSE), methicillin-susceptible Staphylococcus aureus (MSSA) and MRSA, respectivelyMarinopyrrole derivatives as potential antibiotic agents against methicillin-resistant Staphylococcus aureus (II)23955285
MBX2319, a novel pyranopyridineExhibit antibacterial activity in combination with other antibiotics only, decreased the MICs of ciprofloxacin (CIP), levofloxacin, and piperacillin versus E. coli AB1157 by 2-, 4-, and 8-fold, respectivelyMBX2319 is a potent EPI with possible utility as an adjunctive therapeutic agent for the treatment of infections caused by Gram-negative pathogens.24247144
LFF571antibacterial activity against Clostridium difficile is due to inhibition of translationMechanism of action of and mechanism of reduced susceptibility to the novel anti-Clostridium difficile compound LFF571.22644023
liposomal linolenic acid (LipoLLA)potent bactericidal activity against several clinical isolated antibiotic-resistant strains of H. pylori including both the spiral and coccoid formMechanism of antibacterial activity of liposomal linolenic acid against Helicobacter pylor25793403
AB206, nalidixic acid derivativeStrongly inhibits deoxyribonucleic acid (DNA) synthesis in Escherichia coliMode of action of a new nalidixic acid derivative, AB206. A new chemotherapeutic agent, AB206, shows potent antibacterial activity against gram-negative bacteria, including most of the nalidixic acid-resistant strains tested.6156644
Van-M-02, a novel glycopeptidepotent activities against Gram-positive bacteria, including vancomycin-resistant enterococci (VRE) and vancomycin-resistant Staphylococcus aureus (VRSA)Mode of action of Van-M-02, a novel glycopeptide inhibitor of peptidoglycan synthesis, in vancomycin-resistant bacteria.19933802
anacardic acid analogues possessing different side chains viz. phenolic, branched, and alicyclic [6-(4',8'-dimethylnonyl)salicylic acid, and the alicyclic side-chain analogue, 6-cyclododecylmethyl salicylic acid ]Maximun anti MRSA activiry with (MIC) 0.39 microg/mLMolecular design of anti-MRSA agents based on the anacardic acid scaffold17601740
ilamycin congeners (1-6) bearing rare L-3-nitro-tyrosine and L-2-amino-4-hexenoic acid structural unitsminimum inhibitory concentration value ?9.8 nM to Mycobacterium tuberculosis H37RvMost impressively, ilamycins E1/E2, which are produced in high titers by a genetically engineered mutant strain, show very potent anti-tuberculosis activity with an minimum inhibitory concentration value ?9.8 nM to Mycobacterium tuberculosis H37Rv constituting extremely potent and exciting anti-tuberculosis drug leads.28855504
NB2001, (triclosan in a prodrug form with a cephalosporin scaffold)antibacterial activity was studied against beta lactamase producing strainsNANB2001, a novel antibacterial agent with broad-spectrum activity and enhanced potency against beta-lactamase-producing strains. Enzyme-catalyzed therapeutic activation (ECTA) is a novel prodrug strategy to overcome drug resistance resulting from enzyme overexpression. beta-Lactamase overexpression is a common mechanism of bacterial resistance to beta-lactam antibiotics.11959554
NCL195 (4,6-bis(2-((E)-4-methylbenzylidene)hydrazinyl)pyrimidin-2-amine)potent bactericidal activity against Streptococcus pneumoniae and Staphylococcus aureusless cytotoxic to mammalian cell lines than robenidineNCL195 was bactericidal against Acinetobacter spp and Neisseria meningitidis and also demonstrated potent activity against A. baumannii, Pseudomonas aeruginosa, Escherichia coli, Klebsiella pneumoniae and Enterobacter spp. in the presence of sub-inhibitory concentrations of ethylenediaminetetraacetic acid (EDTA) and polymyxin B.28873428
7-[4-(4-(benzoyl)carbopiperazin-1-yl)]piperazinyl derivative 5h and two 7-[4-(4- (benzenesulfonyl)carbopiperazin-1-yl)]piperazinyl derivatives 5k and 5lMIC values as low as 16 ?g/ml against ciprofloxacin-resistant P. aeruginosa (CRPA)New 7-[4-(4-(un)substituted)piperazine-1-carbonyl]- piperazin-1-yl] derivatives of fluoroquinolone: synthesis and antimicrobial evaluation23807580
1beta-methylcarbapenems with thiazol-2-ylthio groups at the C-2 position [SM-197436 , SM-232721, and SM-232724 ]potent antibacterial activity especially against methicillin-resistant staphylococci, vancomycin-resistant enterococci and penicillin-resistant Streptococcus pneumoniaeNew anti-MRSA and anti-VRE carbapenems; synthesis and structure-activity relationships of 1beta-methyl-2-(thiazol-2-ylthio)carbapenems.12374386
7beta-[2-(5-amino-1,2,4-thiadiazol-3-yl)-2-ethoxyiminoacetamido] cephalosporins bearing 4-[3-(aminoalkyl)-ureido]-1-pyridinium at C-3potent antibacterial activity against MRSA and Pseudomonas aeruginosaNew broad-spectrum parenteral cephalosporins exhibiting potent activity against both methicillin-resistant Staphylococcus aureus (MRSA) and Pseudomonas aeruginosa15246098
2-((4-(4,5-dibromo-1H-pyrrole-2-carboxamido)phenyl)amino)-2-oxoacetic acid (9a)IC50 of 0.18 ?M against E. coli gyraseNew N-phenyl-4,5-dibromopyrrolamides and N-Phenylindolamides as ATPase inhibitors of DNA gyrase27100032
Nitric oxideSublethal concentrations of NO inhibited the enzymatic activity of [4Fe-4S]-cofactored aconitase of aerobic and anaerobic B. pseudomallei.Nitric oxide-dependent killing of aerobic, anaerobic and persistent Burkholderia pseudomallei. Burkholderia pseudomallei infections are fastidious to treat with conventional antibiotic therapy, often involving a combination of drugs and long-term regimes.22521523
Nitrosoglutathione generating nitric oxide (NO)Percent survival in the NO-np+GSH -treated isolates was significantly lower than in the a nitric oxide-releasing nanoparticle (NO-np) (36.1% vs 8.3%; P=.004). In addition, NO-np+GSH accelerated wound closure in P aeruginosa-infected wounds, and NO-np+GSH-treated wounds had significantly lower bacterial burden when compared to NO-np-treated wounds (P<.001).Nitrosoglutathione generating nitric oxide nanoparticles as an improved strategy for combating Pseudomonas aeruginosa-infected wounds. Pseudomonas aeruginosa is a community-acquired, nosocomial pathogen that is an important cause of human morbidity and mortality; it is intrinsically resistant to several antibiotics and is capable of developing resistance to newly developed drugs via a variety of mechanisms.23377518
Compounds containing the N-alkyl-N-(pyridin-2-yl)hydroxylamine structurepotent antibacterial activity against the Gram-positive bacterium Micrococcus luteus ATCC 10240 (MIC(90) = 2.0 ?M or 0.41 ?g/mL) and moderate activity against other Gram-positive strains including antibiotic resistant strains of Staphylococcus aureus (MRSA) and Enterococcus faecalis (VRE)N-O chemistry for antibiotics: discovery of N-alkyl-N-(pyridin-2-yl)hydroxylamine scaffolds as selective antibacterial agents using nitroso Diels-Alder and ene chemistry21859126
3-(2-aminothiazol-4-yl)-7-chloro-6-(pyrrolidin-1-yl) quinolone 12bActivity againts methicillin-resistant Staphylococcus aureus (MRSA) by formation of a compound 12b-Cu(2+)-DNA ternary complex in which the Cu(2+) ion acts as a bridge between the backbone of 3-aminothiazolquinolone and the phosphate group of the nucleic acid.low cytotoxicity to hepatocyte cellsNovel 3-Aminothiazolquinolones: Design, Synthesis, Bioactive Evaluation, SARs, and Preliminary Antibacterial Mechanism.27115717
(R)-Hydroxy-1,5-naphthyridinone left-hand side (LHS) oxabicyclooctane linked pyridoxazinone right-hand side (RHS) containing NBTIs showed a potent Gram-positive antibacterial profile. SAR around the RHS moiety, including substitutions around pyridooxazinone, pyridodioxane, and phenyl propenoidsA fluoro substituted pyridoxazinone showed an MIC against Staphylococcus aureus of 0.5 ?g/mL, pyridodioxane-containing NBTI showed a S. aureus MIC of 0.5 ?g/mLNovel bacterial topoisomerase inhibitors (NBTIs) are a new class of broad-spectrum antibacterial agents targeting bacterial Gyrase A and ParC and have potential utility in combating antibiotic resistance.25978963
bis-cyclic guanidinescompromise bacterial membranes without developing resistance, inhibit biofilms formed by E. coli, and exhibit excellent in vivo activity against MRSANovel bis-cyclic guanidines as potent membrane-active antibacterial agents with therapeutic potential. We designed a class of small dimeric cyclic guanidine derivatives which display potent antibacterial activity against both multidrug-resistant Gram-negative and Gram-positive bacteria.29052670
bis-(imidazolinylindole) derivativeseffective against a broad range of gram-positive and gram-negative bacterial species, including several antibiotic-resistant strainsNovel broad-spectrum bis-(imidazolinylindole) derivatives with potent antibacterial activities against antibiotic-resistant strains19635954
fluorinated pyrrolomycinMIC of 73 ng/mL, MBC of 4 ?g/mL, kill staphylococcal-associated biofilm at 8 ?g/mLNovel fluorinated pyrrolomycins as potent anti-staphylococcal biofilm agents.27565555
6-O-substituted and 6,12-di-O-substituted 8a-aza-8a-homoerythromycin A and 9a-aza-9a-homoerythromycin A ketolides and ketolides based on 14-membered erythromycin oxime scaffoldPotent activity against a variety of erythromycin-susceptible and macrolide-lincosamide-streptogramin B (MLS(B))-resistant Gram-positive pathogens as well as fastidious Gram-negative pathogensNovel hybrids of 15-membered 8a- and 9a-azahomoerythromycin A ketolides and quinolones as potent antibacterials.21055953
SKI-356313, new imidazoline scaffoldBactericidal activity against Mycobacterium tuberculosis and Gram-positive cocci, including vancomycin-resistant Enterococcus faecium (VRE) and methicillin-resistant Staphylococcus aureus (MRSA)Novel imidazoline antimicrobial scaffold that inhibits DNA replication with activity against mycobacteria and drug resistant Gram-positive cocci25222597
2-([3-[(1H-benzimidazol-2-ylsulfanyl)methyl]-2-methylphenyl]sulfanyl)ethyl carbamatesMIC(90) = 0.25 microg/mL against H. pylori strainsNovel structures derived from 2-[[(2-pyridyl)methyl]thio]-1H-benzimidazole as anti-Helicobacter pylori agents.12213071
4-chloro-2,6-dimethylphenol analoguesThe most potent analogs have a MIC of 160 to 320 nM against B. anthracis and may target the cytoskeletal protein FtsZOligochlorophens are potent inhibitors of Bacillus anthracis.20566769
Derivatives of 2?{[4?(5?bromo?3?methylpyridin?2?yl)butyl]amino}?1,4?dihydroquinolin?4?oneThe most potent derivative hasexcellent antibacterial activity against staphylococcal and enterococcal pathogens, including strains resistant to clinical antibiotics.Optimisation of aryl substitution leading to potent methionyl tRNA synthetase inhibitors with excellent gram-positive antibacterial activity. Optimisation of the left-hand-side aryl moiety of a file compound screening hit against Staphylococcus aureus methionyl tRNA synthetase led to the identification of a series of potent nanomolar inhibitors.12639554
psammaplin A (1) analoguesantibacterial agents (e.g. 17, 57, 58, 69, and 70), some possessing greater than 50-fold higher activities than the natural product.In fact, the most interesting compound in this study proved to be the heterodimer 58 consisting of a 3?bromo?phenyl alanine subunit and a 4??fluorophenyl moiety, exhibiting a therapeutic index (TI) of 37.5.Optimization and mechanistic studies of psammaplin A type antibacterial agents active against methicillin-resistant Staphylococcus aureus (MRSA). N As described in the preceding article, utilizing a novel combinatorial disulfide exchange strategy, a library of psammaplin A (1) analogues was constructed and screened for antibacterial activity leading to the identification of a collection of diverse lead compounds.11686610
curcumintreatment for Streptococcus agalactiae infectionOur results demonstrated that curcumin dietary supplement exerts potent bactericidal action against S. agalactiae, presenting 100% of therapeutic efficacy when compared to infected and non-supplemented animals.29407233
silver sulfadiazine and silver-coated dressing1% silver sulfadiazine > silver-coated dressing > 3% citric acid > 0.5% chlorhexidine acetate > control group.Our results supported the efficacy of topical therapy by silver sulfadiazine and silver-coated dressing on infections caused by multi-drug resistant Pseudomonas spp.24229034
quaternised chitosan derivative (hydroxypropyltrimethyl ammonium chloride chitosan, HACCOur study indicates that 26%HACC-loaded PMMA prevents biofilm formation of Staphylococcus, including antibiotic-resistant strains, on the surface of bone cement, and downregulates the virulence-associated gene expression of antibiotic-resistant staphylococcus, thus providing a promising new strategy for combating implant infections and osteomyelitis.22014946
IgAOur study provides a mechanistic explanation for the well-documented risk of P. aeruginosa infection following antimicrobial therapy, and we propose local administration of IgA as a novel prophylactic strategy.29771684
5-episinuleptolideanti-biofilm activities against only Gram-negative bacteriaOur study showed potentially synergistic activity of combination therapy with 5-episinuleptolide and levofloxacin against biofilm formation and biofilm cells.27483290
AM-8722, Oxabicyclooctane-Linked Bacterial Topoisomerase Inhibitortargets DNA gyrase and topoisomerase IVOverall, AM-8722 is a selective and potent NBTI that displays broad-spectrum antimicrobial activity in vitro and in vivo.27246784
BAG-S53P4Owing to its osteoconductive, antibacterial and antibiofilm properties, the use of BAG-S53P4 may be a successful strategy for the treatment of bone and prosthetic joint infections.26462989
pestaloneactivity against methicillin-resistant Staphylococcus aureus (MIC = 37 ng/mL) and vancomycin-resistant Enterococcus faecium (MIC = 78 ng/mL)Pestalone, a new antibiotic produced by a marine fungus in response to bacterial challenge11720529
phosphodiesterase-4 (PDE4) inhibitor, CC-3052,"To study the effect of CC-3052 treatment on the ability of INH to kill Mtb in the lungs of infected rabbits, animals were treated from 4 weeks post-infection with high dose INH (50 mg/kg body weight/day) or CC-3052 (25 mg/kg body weight/day), neither or both for 4 or 8 weeks (i.e., 8 or 12 weeks post-infection)."CC-3052, is water soluble, more stable in human plasma and ?200-fold more potent in reducing TNF-? production, compared to the parent drugPhosphodiesterase-4 inhibition alters gene expression and improves isoniazid-mediated clearance of Mycobacterium tuberculosis in rabbit lungs. These findings provide a basis for exploring the potential use of adjunctive immune modulation with PDE4 inhibitors to enhance the efficacy of existing anti-TB treatment.21949656
6-methoxytetrahydro ?-mangostin (16)antimycobacterial activity with minimum inhibitory concentration (MIC) of 0.78 ?g/mLPotent activity against multidrug-resistant Mycobacterium tuberculosis of ?-mangostin analogs23150066
laurinterol and allolaurinterollaurinterol and allolaurinterol displayed potent bactericidal activity against MRSA at 3.13 microg mL(-1) and against vancomycin-susceptible Enterococcus at 3.13 microg mL(-1) and 6.25 microg mL(-1), respectively.Potent antibacterial activity of halogenated compounds against antibiotic-resistant bacteria15549668
Bisbenzimidazole and Carbonyl Cyanide 3-Chlorophenylhydrazone combinationInhibited biofilm formation, eradicate preformed biofilms and kills the biofilm cells of P. aeruginosa.PPEF (bisbenzimidazole) targeting topoisomerase IA is observed to be an effective bactericidal agent against both Gram-positive and Gram-negative bacterial strains and thus can be developed as potent broad-spectrum antibiotic against MDR strains.28303897
Chloro[2,6-bis(1-methyl imidazol)pyrazine]gold(I), 2b and chloro [2,6-bis(1-methyl imidazol)pyrazine]silver(I), 2a complexesInhibit the biofilm formation by Gram-positive bacteria, Streptococcus mutans and Gram-negative bacteria, Escherichia coli, causing drastic damage to the bacterial cell wall and increasing membrane permeabilityPyrazine functionalized Ag(I) and Au(I)-NHC complexes are potential antibacterial agents22680631
Isoamyl- or cyclopropylmethylene-substituted dipyrrole derivativesBinds to minor groove of DNAPyrrole tetraamides are potent antibacterials against vancomycin resistant Enterococci [corrected] and methicillin resistant Staphylococcus aureus. A new series of short pyrrole tetraamides are described whose submicromolar DNA binding affinity is an essential component for their strong antibacterial activity.11831893
benzyloxy, benzylamino, and phenoxy derivatives of 5-phenyl-3-isoxazolecarboxylic acid ethyl estersnanomolar activity against the replicating bacteria (R-TB) and low micromolar activity against the nonreplicating bacteria (NRP-TB)Rational design of 5-phenyl-3-isoxazolecarboxylic acid ethyl esters as growth inhibitors of Mycobacterium tuberculosis. a potent and selective series for further drug development.20000577
2-phenylquinoline derivativesS. aureus NorA efflux pump inhibitors (EPIs)Re-evolution of the 2-phenylquinolines: ligand-based design, synthesis, and biological evaluation of a potent new class of Staphylococcus aureus NorA efflux pump inhibitors to combat antimicrobial resistance23710549
ResazurinAt concentration of 44 ?M, a potent bactericidal effect was observed against various Francisella and Neisseria species, including the human pathogens type A F. tularensis (Schu S4) and N. gonorrhoeae.Replication of F. tularensis in primary human macrophages and non-phagocytic cells was abolished following treatment with 44 ?M resazurin indicating this compound could be an effective therapy for tularemia in vivo24367766
auranofinPotent antibacterial activity against all tested strains of S. aureus, including meticillin-resistant S. aureus (MRSA), vancomycin-intermediate S. aureus (VISA) and vancomycin-resistant S. aureus (VRSA), with minimum inhibitory concentrations (MICs) ranging from 0.0625?g/mL to 0.125?g/mLRepurposing auranofin for the treatment of cutaneous staphylococcal infections26895605
stannous fluoride (SnF2) dentifrice (SSF)broad antimicrobial activity against both Gram-positives and Gram-negatives and, in particular, has potent activity against Streptococcus mutansResults of in vitro time-kill experiments with representative oral bacteria demonstrated that SnF2 exerts broad antimicrobial activity against both Gram-positives and Gram-negatives and, in particular, has potent activity against Streptococcus mutans.8593200
BPT L-159,061 (Biphenyl tetrazoles)Inhibition of metallo-beta-lactamase by binding to two zinc atoms in the active siteRESULTS: Biphenyl tetrazoles (BPTs) are a structural class of potent competitive inhibitors of metallo-beta-lactamase identified through screening and predicted using molecular modeling of the enzyme structure.9545432
RetinoidsBenzoyl peroxide (BPO) is a nonantibiotic antibacterial agent that is highly effective against P acnes and for which no resistance against it has been detected to date.Retinoids are important components in combination therapy for acne, including use with antibiotics, and can serve as an alternative to these agents in maintenance therapy.17649854
SCE-129 [3-(4-carbamoyl-1-pyridiniomethyl)-7beta-(d-alpha-sulfophenylacetamido)-ceph-3-em -4-carboxylate monosodium salt]Active against Pseudomonas aeruginosa and some gram-positive bacteriaSCE-129, antipseudomonal cephalosporin: in vitro and in vivo antibacterial activities. SCE-129 [3-(4-carbamoyl-1-pyridiniomethyl)-7beta-(d-alpha-sulfophenylacetamido)-ceph-3-em -4-carboxylate monosodium salt], a new semisynthetic cephalosporin, shows potent in vitro antibacterial activities against Pseudomonas aeruginosa and some gram-positive bacteria, whereas it shows lower activity against many gram-negative rods.417670
8-hydroxyquinoline (8HQ)Cu-dependent bactericidal inhibitor with MIC in the presence of Cu 0.16 ?M for replicating and nonreplicating Mycobacterium tuberculosis cells.Screening for Cu toxicity-enhancing antibacterial molecules identified 8-hydroxyquinoline (8HQ) to be a potent Cu-dependent bactericidal inhibitor of Mycobacterium tuberculosis .27431227
?-mangostin and ceftazidimeTime-kill curves showed that the AMT/CTZ combination was significantly more efficient (P < 0?01) at reducing CRAB than the individual components.: The data suggest that AMT in combination with CTZ is synergistic and efficient against CRAB.?-mangostin has no cytotoxic effects.Sep 3. Synergy and mechanism of action of ?-mangostin and ceftazidime against ceftazidime-resistant Acinetobacter baumannii. Pimchan T(1), Maensiri D(1), Eumkeb G(2). Author information: (1)School of Biology, Institute of Science, Suranaree University of Technology, Nakhon Ratchasima, Thailand. (2)School of Preclinic, Institute of Science, Suranaree University of Technology, Nakhon Ratchasima, Thailand. To address the resistance of Acinetobacter baumannii to ?-lactam antibiotics, combination therapy between different antibiotic classes is increasingly used.28799218
Cell-penetrating peptide (P3 and P8) and antibiotic combinationlower the MICs against oxacillin, norfloxacin, and vancomycin to susceptible levelsno significant hemolytic activitySimultaneously, time-kill kinetics revealed the increased uptake of antibiotics. In summary, CPPs assist to restore the effectiveness of antibiotics at much lower concentration, eliminate the antibiotic toxicity, and represent the CPP-antibiotic combination therapy as a potential novel weapon to combat MRSA infections.26837216
2-phenylquinoline efflux inhibitor (4-(2-(piperazin-1-yl)ethoxy)-2-(4-propoxyphenyl) quinolone - PQQ4R)destabilization of the E. coli inner membrane potential and ATP production impairment, ultimately leading to efflux pump inhibition by interference with the energy required by the efflux systemsSince drug resistance mediated by the activity of efflux pumps depends largely on the proton motive force (PMF), dissipaters of PMF such as PQQ4R, can be regarded as future adjuvants of conventional therapy against E. coli and other Gram-negative bacteria, especially their multidrug resistant forms.28516003
3-(4-(N,N-Dimethylaminomethyl)phenyl)quinoline derivativesMost compounds have IC50 values between 20 and 40 ?m,Structural Simplification of Bedaquiline: the Discovery of 3-(4-(N,N-Dimethylaminomethyl)phenyl)quinoline-Derived Antitubercular Lead Compounds. Bedaquiline (BDQ) is a novel and highly potent last-line antituberculosis drug that was approved by the US FDA in 2013.27792278
halogenated phenazines (HP)Halogenated phenazine 14 proved to be the most potent biofilm-eradicating agent (?99.9% persister cell killing) against MRSA (MBEC < 10 ?M), MRSE (MBEC = 2.35 ?M), and VRE (MBEC = 0.20 ?M) biofilms while 11 and 12 demonstrated excellent antibacterial activity against M. tuberculosis (MIC = 3.13 ?M).Structure-Activity Relationships of a Diverse Class of Halogenated Phenazines That Targets Persistent, Antibiotic-Tolerant Bacterial Biofilms and Mycobacterium tuberculosis.27018907
6 beta-(2-aryl-2-sulfoacetamido)-6 alpha-methoxy penicillanic acidspotent activity against Pseudomonas aeruginosa including beta-lactamase producing strainsStructure-activity studies of these derivatives bearing hydrophilic substituents in the phenyl ring led to the identification of disodium 6 beta-[D-2-(3,4-dihydroxyphenyl)-2-sulfoacetamido]-6 alpha-methoxypenicillanate (2m) as a compound with potent activity against Pseudomonas aeruginosa including beta-lactamase producing strains.3096924
7-((2-thiazol-2-yl)benzimidazol-1-yl)-2,4 diaminoquinazolinePotent inhibitor of S. aureus DHFR (Ki = 0.002 nM), antibacterial potency against S. aureus with MIC of 0.0125 ?g/mL and trimethoprim-resistant S. aureus (MIC 0.25 ?g/mL)Structure-based design of new dihydrofolate reductase antibacterial agents: 7-(benzimidazol-1-yl)-2,4-diaminoquinazolines24428639
suraminSuramin is a potent and selective inhibitor of Mycobacterium tuberculosis RecA protein and the SOS response: RecA as a potential target for antibacterial drug discovery.24722837
6?-amino-6?-N-[(S)-4-amino-2-hydroxybutyryl]-6?-deoxyarbekacin (6o)antibacterial activity against S. aureusSynthesis and antibacterial activity of 4? or 6?-alkanoylamino derivatives of arbekacin.25990952
HMR 3647 a new ketolidepotent activity against erythromycin susceptible and resistant pathogens, including penicillin G/erythromycin A-resistant S. pneumoniae and H. influenzae.Synthesis and antibacterial activity of HMR 3647 a new ketolide highly potent against erythromycin-resistant and susceptible pathogens. In the search for new ketolides with improved activities against erythromycin-resistant S. pneumoniae and H. influenzae we synthesized a new 11,12 carbamate ketolide substituted by an imidazo-pyridyl side chain: HMR 3647.10560728
4''-O-carbamoyl erythromycin-A derivativesDerivatives 4c-4e and 4g had most potent activity against all the tested erythromycin-susceptible strains, derivatives 4e and 4g were the most effective against erythromycin-resistant S. pneumoniae encoded by the mef gene (0.25 and 0.25 microg/mL), derivatives 4a and 4b exhibited significantly improved activity against erythromycin-resistant S. pneumoniae encoded by the erm gene.Synthesis and antibacterial activity of novel 4''-O-carbamoyl erythromycin-A derivatives20803622
N-[2-(coumarin-3-yl)-2-oxoethyl]ciprofloxacin derivative (compound 8b)antibacterial activity against some gram-positive and gram-negative bacteria, including methicillin-resistant Staphylococcus aureus (MRSA)Synthesis and antibacterial activity of quinolone-based compounds containing a coumarin moiety18072241
4?-glycyl linked quinolyl-azithromycinsPost potent derivatives have activity against Moraxella catarrhalis, inducibly MLSB resistant Staphylococcus aureus, clinically important respiratory tract pathogens, including erythromycin-susceptible and MLSB resistant strains of Streptococcus pneumoniae, Streptococcus pyogenes, and Haemophilus influenzaeSynthesis and antibacterial evaluation of novel 4?-glycyl linked quinolyl-azithromycins with potent activity against macrolide-resistant pathogens.26860929
macrocyclic ?-hairpin-shaped peptidomimeticsActivity against Pseudomonas aeruginosaSynthesis and antimicrobial activity against Pseudomonas aeruginosa of macrocyclic ?-hairpin peptidomimetic antibiotics containing N-methylated amino acids27240465
RP60556A, benzo[b]naphthyridones compoundbactericidal multiresistant Staphylococcus aureusSynthesis and biological evaluation of benzo[b]naphthyridones, a series of new topical antibacterial agents.11294391
indole core-based derivativesin vitro inhibition of different Gram-positive bacteria, Gram-negative and multi drug resistant pathogensSynthesis and biological evaluation of indole core-based derivatives with potent antibacterial activity against resistant bacterial pathogens. The emergence of drug resistance in bacterial pathogens is a growing clinical problem that poses difficult challenges in patient management.28465626
quinolone (S)-9-fluoro-10-(4-hydroxypiperidin-1-yl)-3-methyl-7-oxo-3,7-dihydro-2H-[1,4]oxaz ino[2,3,4-ij]quinoline-6-carboxylic acid L-arginine tetrahydrateAntimicrobial activity against methicillin-resistant Staphylococcus aureus clinical isolates, penicillin-resistant Streptococcus pneumoniae clinical isolates, and Streptococcus pyogenesSynthesis and biological evaluation of levofloxacin core-based derivatives with potent antibacterial activity against resistant Gram-positive pathogens.26238324
3-O-chlorobenzyl (3-O-arylalkyl-2,6-difluorobenzamide derivatives)3-O-chlorobenzyl derivative 36 was the most effective in antibacterial activity (0.5, 4, and 8 ?g/mL) against Bacillus subtilis ATCC9372, methicillin-resistant Staphylococcus aureus ATCC29213, and penicillin-resistant Staphylococcus aureus PR, while 3-O-methylbenzyl derivative 41 only exhibited the most potent activity (2 ?g/mL) against Staphylococcus aureus ATCC25923.Synthesis and Biological Evaluation of Novel FtsZ-targeted 3-arylalkoxy-2,6-difluorobenzamides as Potential Antimicrobial Agents26348110
Rhodanine derivatives bearing a quinoline moiety (6a-h, 7a-g, and 8a-e)The most effective derivative has minimum inhibitory concentration (MIC) values of 1 ?g/mL against multidrug-resistant Gram-positive organisms, including methicillin-resistant and quinolone-resistant Staphylococcus aureus (MRSA and QRSA, respectively)compounds 6g, 7g and 8e exhibited in vitro antibacterial activity at non-cytotoxic concentrations.Synthesis and biological evaluation of rhodanine derivatives bearing a quinoline moiety as potent antimicrobial agents.23787100
Dibasic tetrahydropyran-based compoundspotent inhibitors of both DNA gyrase and topoisomerase IV, displaying antibacterial activities against Gram-positive and Gram-negative pathogens (Staphylococcus aureus, Enterobacteriaceae, Pseudomonas aeruginosa, and Acinetobacter baumannii)Synthesis and Characterization of Tetrahydropyran-Based Bacterial Topoisomerase Inhibitors with Antibacterial Activity against Gram-Negative Bacteria.28406300
5''-modified neomycin derivativesSynthesis and combinational antibacterial study of 5''-modified neomycin. A library of 5''-modified neomycin derivatives were synthesized for an antibacterial structure-activity optimization strategy.19629142
2-acetamido-2-deoxy-?-D-glucopyranosyl N,N-dimethyldithiocarbamate (OCT313, Glc-NAc-DMDC) and its derivativesGlc-NAc-pyrrolidine dithiocarbamate (OCT313HK, Glc-NAc-PDTC) exhibited the most potent anti-tubercular activity with the minimal inhibitory concentration (MIC) of 6.25-12.5 ?g/ml.Synthesis and evaluation of anti-tubercular activity of new dithiocarbamate sugar derivatives21232949
Galf N,N-didecyl sulfenamide 8d(MIC) of 1 microg/mL in a cell based assay against a representative strain of Mycobacterium smegmatisSynthesis and evaluation of galactofuranosyl N,N-dialkyl sulfenamides and sulfonamides as antimycobacterial agents17303419
4,4'-bis-[2-(6-N-substituted-amidino)indolyl] diphenyl etherActivity against drug resistant bacterial strains MRSA, MRSE and VRESynthesis and in vitro activity of dicationic indolyl diphenyl ethers as novel potent antibiotic agents against drug-resistant bacteria.28109787
5-hydroxy-5-trifluoromethyl-4,5-dihydro-1H-1-(isonicotinoyl)-pyrazole (2a) and 5-hydroxy-3-(4-methylphenyl)-5-trifluoromethyl-4,5-dihydro-1H-1-(isonicotinoyl) pyrazole (2d)Inhibitors of mycolic acid biosynthesis, active against susceptible M. tuberculosis and several INH-resistant strainsSynthesis and in vitro antimycobacterial activity of 3-substituted 5-hydroxy-5-trifluoro[chloro]methyl-4,5-dihydro-1H-1-(isonicotinoyl) pyrazoles18571384
1-(4-fluorophenyl)-3-(4-{1-[(pyridine-4-carbonyl)-hydrazono]ethyl}phenyl)thiourea (4d)minimum inhibitory concentration of 0.49 microM against M. tuberculosis H37Rv and INH-resistant M. tuberculosis.Synthesis and in vitro antitubercular activity of some 1-[(4-sub)phenyl]-3-(4-{1-[(pyridine-4-carbonyl)hydrazono]ethyl}phenyl)thiourea16303302
oxazolidinone-class antimicrobial agents with 5-substituted octahydrocyclopenta[c]pyrrole moieties at the C-ring of linezolid and an acetamide or 1,2,3-triazole ring as the C-5 side chain of the oxazolidinone ringActive against some resistant Gram-positive and -negative bacteria, derivatives like endo-alcohol 2a and exo-alcohol 2b showed potent inhibitory activity against M. tuberculosis H37Rv, several analoguess showed potent in vitro antibacterial activity against vancomycin-resistant bacteria and s linezolid-resistant methicillin-resistant Staphylococcus aureus (MRSA) strains.Synthesis and in vitro evaluation of the antitubercular and antibacterial activity of novel oxazolidinones bearing octahydrocyclopenta[c]pyrrol-2-yl moieties.25297523
1,2-disubstituted-1H-benzimidazole-N-alkylated-5-carboxamidine derivativesDerivatives with 3,4-dichloro substituted phenyl at the position C-2, of N-bulky alkyl substituted benzimidazolecarboxamidines exhibited the greatest activity with MIC values of 1.56-0.39 microg/ml.Synthesis and potent antibacterial activity against MRSA of some novel 1,2-disubstituted-1H-benzimidazole-N-alkylated-5-carboxamidines.15992965
4-(5, 6-dichloro-1H-benzimidazol-2-yl)-N-substituted benzamidesHighest antibacterial activity was achieved with with MIC values of 3.12 microg/mL against S. aureus, MRSA and MRSESynthesis and potent antimicrobial activity of some novel 4-(5, 6-dichloro-1H-benzimidazol-2-yl)-N-substituted benzamides.15476288
[1-(2,4-dichlorobenzyl)-N- (2-diethylaminoethyl)-1H-benzimidazole-5-carboxamidine], with a 3,4-dichlorophenyl group at the C-2 positionMIC = 3.12 microg/mL against both some bacteria and the fungus C. albicansSynthesis and potent antimicrobial activity of some novel N-(alkyl)-2-phenyl-1H-benzimidazole-5-carboxamidines. A series of 22 novel 1,2-disubstituted-1H-benzimidazole-N-alkylated-5- carboxamidine derivatives were synthesized and evaluated for in vitro antibacterial activity against S. aureus and methicillin resistant S. aureus (MRSA), E. coli, E. faecalis and for antifungal activity against C. albicans.18007533
1H-benzimidazolecarboxamidinesThe most potent compound (32) has minimal inhibitory concentrations value 0.78 ?g/mL).Synthesis and potent in vitro activity of novel 1H-benzimidazoles as anti-MRSA agents.22497759
1beta-methyl-2-(naphthosultamyl)methyl-carbapenems (L-786,392)potent anti-MRSA activitySynthesis and properties of 2-(naphthosultamyl)methyl-carbapenems with potent anti-MRSA activity: discovery of L-786,392. A series of 1beta-methyl-2-(naphthosultamyl)methyl-carbapenems bearing dicationic groups on the naphthosultamyl moiety was prepared and evaluated for activity against resistant gram-positive bacteria.10201828
dicationic diaryl ethersThe most potentcompound had anti-MRSA MIC value of 0.06 microg/mLSynthesis and structure-activity relationship of dicationic diaryl ethers as novel potent anti-MRSA and anti-VRE agents19589676
2-pyridones (pyrido[1,2-alpha]pyrimidine and quinolizine)DNA gyrase inhibitorSynthesis and structure-activity relationships of 2-pyridones: a novel series of potent DNA gyrase inhibitors as antibacterial agents. Two novel series of 2-pyridones were synthesized by transposition of the nitrogen of 4-quinolones to the bridgehead position.8759628
7-[(3S,4R)-4-(1-aminocyclopropan-1-yl)-3-fluoropyrrolidin-1-yl] derivative 3 (=DQ-113)Activity against clinically isolated resistant pathogensSynthesis and structure-activity relationships of 5-amino-6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-8-methylquinolonecarboxylic acid antibacterials having fluorinated 7-[(3R)-3-(1-aminocyclopropan-1-yl)pyrrolidin-1-yl] substituents.12620077
lincomycin analogs modified at the 6- and 7-positionsantibacterial activity against different bacteriaSynthesis and structure-activity relationships of novel lincomycin derivatives28559581
2''-amino-2''-deoxyarbekacinActive against methicillin-resistant Staphylococcus aureusSynthesis of 2''-amino-2''-deoxyarbekacin and its analogs having potent activity against methicillin-resistant Staphylococcus aureus. Based on our studies on the enzymatic modifications of arbekacin by methicillin-resistant Staphylococcus aureus (MRSA), replacement of the 2''-hydroxyl group by an amino group in arbekacin was designed to synthesize derivatives that would be active against MRSA. 2''-Amino-2''-deoxyarbekacin and five analogs were synthesized starting from dibekacin.8071128
T-3761, a new fluoroquinoloneThe MIC against methicillin-susceptible Staphylococcus aureus, methicillin-susceptible and -resistant Staphylococcus epidermidis, and Clostridium spp were 0.39 to 6.25 micrograms/ml, aginst streptococci and enterococci tested were 3.13 to 100 micrograms/mlT-3761 had a broad spectrum of activity and had potent activity against gram-positive and -negative bacteria.1332594
T-3912, a novel non-fluorinated topical quinolonein vitro activity of T-3912 against methicillin-susceptible Staphylococcus aureus, ofloxacin-resistant and methicillin-resistant S. aureus, Staphylococcus epidermidis, ofloxacin-resistant S. epidermidis, penicillin-resistant Streptococcus pneumoniae and Propionibacterium acnes was four-fold to 16 000-fold greater than that of other agents at the MIC90 for the clinical isolateT-3912 exhibited more potent bactericidal activity against S. aureus and P. acnes than nadifloxacin and clindamycin in a short time period.11864945
TP-434, a novel fluorocyclineMIC of TP-434 (0.063 ?g/ml), potent inhibition in E. coli in vitro transcription/translation (50% inhibitory concentration [IC(50)] = 0.29 ? 0.09 ?g/ml) and [(3)H]tetracycline ribosome-binding competition (IC(50) = 0.22 ? 0.07 ?M) assays.Target- and resistance-based mechanistic studies with TP-434, a novel fluorocycline antibiotic22354310
2-hydroxy-N'-{[5-(2-nitrophenyl)-2-furyl]methylene}benzohydrazide (B8I-2)inhibited intracellular growth of B. abortus 2308 in J774 macrophages at relatively low ?M concentrations.Targeting bacterial virulence functions in order to disarm pathogens represents a promising alternative to classical antibiotic therapy.21173315
tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide (THPP) and N-benzyl-6',7'-dihydrospiro[piperidine-4,4'-thieno[3,2-c]pyran] (Spiro) analoguesreduce >2 logs bacterial cfu counts in the lungs of infected miceTetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide and N-benzyl-6',7'-dihydrospiro[piperidine-4,4'-thieno[3,2-c]pyran] analogues with bactericidal efficacy against Mycobacterium tuberculosis targeting MmpL323613759
ketolides (6-O-methyl-3-oxoerythromycin derivatives)active against penicillin/erythromycin-resistant pneumococci and noninducers of MLSB resistanceThe 11,12-substituted ketolide 61 (HMR 3004) demonstrated a potent activity against multiresistant pneumococci associated with a well-balanced activity against all bacteria involved in respiratory infections including H. influenzae, Mycoplasma catarrhalis, group A streptococci, and atypical bacteria. In addition HMR 3004 displayed high therapeutic activity in animals infected by all major strains, irrespective of their resistance phenotype.9767644
8-substituted-9,1-[(N-methylimino)methano]- 7-fluoro-5-oxo-5H-thiazolo[3,2-alpha]-quinoline-4-carboxylic acids 5a-qActive against methicillin-resistant Staphylococcus aureus isolates (MRSA)The 8-(4-alkyl-1-piperazinyl) derivatives 5g, 5h, 5j, and 5n provided good oral efficacy and exhibited more potent activity than ofloxacin (6) against the systematic infection with S. aureus IID 803 in mice.8126698
FK037MIC90s: Streptococcus pyogenes (0.012 ?g/ml), Escherichia coli (0.05 ?g/ml ), Streptococcus pneumoniae (0.1 ?g/ml), Klebsiella pneumoniae (0.39 ?g/ml)The advantages of in vitro activity of FK037 were as follows: (1) a broad-spectrum antibacterial activity, (2) the most potent activity (MIC90: 25 micrograms/ml) of the cephalosporins tested against highly methicillin-resistant Staphylococcus aureus (H-MRSA), (3) a strong activity against Enterobacter spp. and Citrobacter freundii resistant to the third-generation cephalosporins tested.8205935
teicoplanin and caffeic acid phenethyl ester (CAPE)The combination of an antioxidant / anti-inflammatory agent, CAPE, added to standard antibiotic therapy might be effective in the treatment of post-sternotomy mediastinitis due to MRSA. DOI: 10.1179/joc.2006.18.3.26817129837
combination of nebulized sodium nitrite and colistimethateSodium nitrite has antimicrobial properties and has been tolerated as a nebulized compound at high concentrations in human subjects with pulmonary hypertensionThe combination of nebulized sodium nitrite and colistimethate may provide a novel therapy for chronic P. aeruginosa airway infections, because sodium nitrite, unlike other antibiotic respiratory chain "poisons," can be safely nebulized at high concentration in humans. .25229185
tobramycin-fumarate combinationEnhanced killing of up to 6 orders of magnitude of P. aeruginosa persisters over a range of CF isolates, including mucoid and nonmucoid strains, was observed for the tobramycin-fumarate combination compared to killing with tobramycin alone. Furthermore, significant fumarate-mediated potentiation was seen in the presence of azithromycin or CF patient sputum.Fumarate also reduced the cytotoxicity of tobramycin-treated P. aeruginosa to human epithelial airway cells.The combination of the aminoglycoside tobramycin with fumarate as an antibacterial potentiator utilizes an antipersister strategy that is aimed at reducing recurrent Pseudomonas aeruginosa infections by enhancing the killing of P. aeruginosa persisters.28923873
PC190723, synthetic antibacterialsefficacious in an in vivo model of infection,The data validate FtsZ as a target for antibacterial intervention and identify PC190723 as suitable for optimization into a new anti-staphylococcal therapy.18801997
1,3-benzoxazol-2(3H)-one derivativesantibiofilm activity against Pseudomonas aeruginosa PA01The discovery that many bacteria use quorum sensing (QS) to regulate their virulence factor and pathogenicity production makes the QS system an attractive target for antimicrobial therapy.22588631
N-thiolated ?-lactamsN-thiolated ?-lactams are FAS-inhibiting antimicrobialsNo reported toxicity.The impact of fatty acids on the antibacterial properties of N-thiolated ?-lactams. Bacterial fatty acid synthesis (FAS) is a potentially important, albeit controversial, target for antimicrobial therapy.21821415
BO-2727, new carbapenemMIC90 ? 0.5 microgram/ml against methicillin-susceptible staphylococci and streptococci, 4 to 8 micrograms/ml Against methicillin-resistant staphylococci, 0.006 to 2 micrograms/ml against members of the family Enterobacteriaceae, Haemophilus influenzae, and Moraxella catarrhali, 2 micrograms/ml against Pseudomonas aeruginosa (imipenem-susceptible strains)The in vivo efficacy of BO-2727 against experimental septicemia caused by gram-positive and gram-negative bacteria, including methicillin-resistant Staphylococcus aureus and imipenem-resistant P. aeruginosa, reflected its potent in vitro activity and high levels in plasma.7625784
S-4661MIC90 0.5 ?g/ml or less against methicillin-susceptible staphylococci and streptococci, 8 ?g/ml against imipenem-resistant Pseudomonas aeruginosaThe in vivo efficacy of S-4661 against experimentally induced infections in mice caused by gram-positive and gram-negative bacteria, including penicillin-resistant Streptococcus pneumoniae and drug-resistant P. aeruginosa, reflected its potent in vitro activity and high levels in plasma in mice.9449267
berberine and 5'-methoxyhydnocarpin (5'-MHC)The inhibitor was identified as 5'-methoxyhydnocarpin (5'-MHC), previously reported as a minor component of chaulmoogra oil, a traditional therapy for leprosy.10677479
antibiotics in combination with silver nanoparticlesThe majority of synergistic effects were observed for combinations of AgNPs given together with gentamicin, but the highest enhancement of antibacterial activity was found with combined therapy together with penicillin G against Actinobacillus pleuropneumoniae.26832810
benzo[b]thiophene-2-boronic acidinhibitors of AmpC beta-lactamaseThe most potent of these compounds, benzo[b]thiophene-2-boronic acid , has an affinity for E. coli AmpC of 27 nM.9804697
MUT056399active against methicillin-susceptible and resistant S. aureus , linezolid-resistant, and multidrug-resistant strains, with MIC(90)s between 0.03 and 0.12 ?g/ml; and MIC(90)s between 0.12 and 4 ?g/ml against coagulase-negative staphylococci, withThe MUT056399 inhibitor of FabI is a new antistaphylococcal compound.21825292
BO-3482, a novel dithiocarbamate carbapenemActive against methicillin-resistant Staphylococcus aureusThe potent in vivo activity of BO-3482-cilastatin against such MRSA infections can be ascribed to the good in vitro anti-MRSA activity and improved pharmacokinetics in mice when BO-3482 is combined with cilastatin and to the bactericidal nature of the carbapenem.9333062
LY333328MIC90 2 microg/ml in Mueller-Hinton II (MH II) broth and 1 microg/ml in brain heart infusion (BHI) brothThe prolonged PAE of LY333328, a potent new bactericidal glycopeptide, and its synergy with ampicillin in a large proportion of strains suggest that further evaluation of this drug in pharmacokinetic studies and experimental infections, including those with VRE, is warranted.9756756
combinations of SIPI-8294 and ?-lactam antibioticsThe research indicates that it may be a promising strategy for combating MRSA infections with the combinations of SIPI-8294 and ?-lactam antibiotics.27173151
coumermycinActive against methicillin-resistant strains of Staphylococcus aureusThe results indicate that coumermycin is potent against MRSA with activity equal or superior to comparable agents in various experimental mouse infections.3492342
benzimidazole Y-754The minimum inhibitory concentration of Y-754 against H. pylori, at 0.025 microg/mlThe results obtained lead to the expectation that the new benzimidazole Y-754 will, in the near future, be used for H. pylori eradication therapy in peptic ulcer patients.15160301
CefepimeCefepime 2 g every 12 hoursonly 3% of patients in each group discontinued therapy because of an adverse event. The most common adverse events were headache, diarrhea, nausea, vomiting, pruritus, and rash.The results of this study indicate that cefepime is a promising, effective, and safe single-agent therapy for serious infections in hospitalized patients.8678098
?-Ag 2 MoO 4 microcrystalsThe silver molybdate was obtained by the conventional hydrothermal method, and the structural, vibrational and morphological properties of the sample were determined using X-ray diffraction, Raman spectroscopy and scanning electron microscopy images.these silver molybdates present a clinically relevant antibacterial activity and enhanced the antibiotic activity of some antibiotics against MDR strain of S. aureus and E. coli, being an interesting alternative to combat antibiotic-resistant bacterial infectious agents.The reversion of antibiotic resistance by combinations with Ag2MoO4 could be a novel strategy to combat infections caused by multiple drug resistance (MDR) pathogens.28006749
tobramycinEighty milligrams of a tobramycin solution were inhaled twice daily after physiotherapy via a jet nebulizer.No evidence of ototoxicity or renal damage was observed.The study demonstrates the safety and clinical efficacy of long-term tobramycin aerosol therapy.2494640
12-oxime and O-oxime ether derivatives of dehydroabietic acidThe most potent derivative has MIC of 0.39-0.78?g/mL against S. aureus Newman, some others have MIC values 1.25-3.13?g/mL aginst multidrug-resistant S. aureusThe synthesis and antistaphylococcal activity of dehydroabietic acid derivatives: Modifications at C-12.27777007
third-generation P-glycoprotein inhibitor tariquidaraddition of tariquidar resulted in a 10-fold reduction of the ciprofloxacin MIC Staphylococcus aureus 1199B (SA1199B)The third-generation P-glycoprotein inhibitor tariquidar may overcome bacterial multidrug resistance by increasing intracellular drug concentration.21393173
titanium dioxide (TiO2)Strain: methicillin resistant Staphylococcus aureus (MRSA 27065)The TiO(2) coating with integrated copper ions could offer a new strategy for preventing implant-associated infections, with antibacterial properties not only against the most common bacteria causing implant infections but also against multiresistant strains such as MRSA.21188483
isosorbide mononitrate (ISMN)Specifically, exposure to ISMN significantly enhanced the efficacy of ciprofloxacin by reducing the number of CFU (~3log10 or ~2log10) of biofilm-associated and planktonic bacteria respectively, compared to drug alone.NAThe use of nitric oxide (NO), a naturally occurring antimicrobial agent, as an alternative strategy to combat bacterial biofilms has recently gained considerable momentum in light of the global threat of emerging antibiotic resistance.29305985
verapamil and Q203 combinationsTherefore, the combination of verapamil and Q203 may be a promising combinatorial strategy for anti-TB treatment to accelerate the elimination of M. tuberculosis.28416541
liposomal BiEDT-tobramycin (LipoBiEDT-TOB)MIC of LipoBiEDT-TOB (0.25mg/L vs. 1024 mg/L). At 4 mg/L vs. 4096 mg/L eradicated highly resistant P. aeruginosa (PA-48913)LipoBiEDT-TOB was significantly less toxic when compared to the free BiEDT, as evaluated by the MTT and LDH assay.These data suggest that the novel LipoBiEDT-TOB drug delivery system could be utilized as a new strategy to enhance the efficacy of existing antibiotics against resistant organisms that commonly affect individuals with chronic lung infections.18448284
titanium dioxide (TiO2)These findings suggest the created materials with high bacterial interaction ability might be a useful strategy to improve the antimicrobial activity of visible-light-activated TiO2.19272171
psammaplin A analogueactive against methicillin-resistant Staphylococcus aureus (MRSA)These psammaplin A analogues were screened directly against various gram positive bacterial strains leading to the discovery of a series of potent antibacterial agents active against methicillin-resistant Staphylococcus aureus (MRSA).11686609
GAR-936, new glycylcyclineMIC against different bacteria: Streptococcus pneumoniae (MIC90, 0.03 ?g/ml), Enterococcus spp. (MIC90, 0.12 or 0.25 ?g/mL), Staphylococcus aureus (MIC50 0.25 ?g/mL), Acinetobacter spp. (MIC90, 2 ?g/mL), Stenotrophomonas maltophilia (MIC90, 4 ?g/mL), Pseudomonas aeruginosa (MIC50, 8 ?g/mL), Haemophilus influenzae (MIC90, 1-2 ?g/mL), Moraxella catarrhalis (MIC90, 0.12 ?g/mL), and various Neisseria spp. (MIC90, 0.12-0.5 ?g/mL)These results indicate that GAR-936 has potent in vitro activity against a wide range of clinically important pathogenic bacteria, and that several gram-positive and -negative isolates resistant to older tetracyclines and other drug classes remain susceptible to GAR-936, the newest glycylcycline candidate for clinical use.10744364
tannic acidThe MICs of EtBr and antibiotics were significantly reduced in the presence of tannic acid, inhibition against the efflux pumps of both strains with a three-fold reduction of the MIC. Bacteria : Staphylococcus aureusNAThese results indicate the possible usage of tannic acid as an adjuvant in antibiotic therapy against multidrug resistant bacteria (MDR).27057677
tannic acidThe MICs of EtBr and antibiotics were significantly different in the presence of tannic acid, indicating the inhibitory effect of this product against efflux pumps of both strains.These results indicate the possible usage of tannic acid as an inhibitor and an adjuvant in the antibiotic therapy against multidrug resistant bacteria (MDR). Copyright ? 2017 Elsevier Inc.28841421
CS-834, a new oral carbapenem which is an ester-type prodrug of R-95867bactericidal activity against Staphylococcus aureus and Escherichia coli.These results suggest that CS-834 may be effective in the therapy of various bacterial infections.9818740
Gallium CitrateMIC against K. pneumoniae ranged from 0.125 to 2.0 ?g/ml GaCi.These results suggest that with more preclinical testing, a topical application of GaCi may be a promising alternative treatment strategy for K. pneumoniae SSTI.26239978
methyl-1,4-hydroquinone and 2,3-dimethyl-1,4-hydroquinone analogues synthesized by amination with amino-?-lactam structuresinhibited the growth of several Gram-positive bacterial strains including multidrug-resistant Staphylococcus aureus and EnterococciThirty-eight potential 1,2- and 1,4-hydroquinoid laccase substrates were screened for their antibacterial and cytotoxic activity to select the best substrates for laccase-catalyzed coupling reaction resulting in potent antibacterial derivatives.26780358
AU-FQ hybrid compound 251D (anilinouracils (AUs) such as 6-(3-ethyl-4-methylanilino)uracil (EMAU) and fluoroquinolones)active against a broad panel of antibiotic-resistant gram-positive pathogens as well as several gram-negative organismslacked toxicity in vitroThis class of AU-FQ hybrids provides a promising new pharmacophore with an unusual dual mechanism of action and potent activity against antibiotic-sensitive and -resistant gram-positive pathogens.17074800
SYN987, SYN1193, and SYN1253Active against streptococci (including penicillin resistant Streptococcus pneumoniae), enterococci and Staphylococcus aureusThis study demonstrates that SYN 987, 1193 and 1253 are extremely potent antibacterial agents which deserve further evaluation.8537267
Azole drugsMIC values of <0.2 and 0.3 micro M, respectively for the drugs econazole and clotrimazoleThis suggests that azole drug therapy may provide a novel antibiotic strategy against strains of M. tuberculosis that have already developed resistance to isoniazid and other front-line drugs.12368427
Vertex aminobenzimidazole VT12-008911MIC(50), MIC(90) and MIC range of VT12-008911 were 0.064, 0.125 and ?0.002-0.25 mg/L, respectivelyTime-kill curve analysis showed that VT12-008911 exhibited potent time-dependent bactericidal activity, at or very close to the MIC, against N. gonorrhoeae.24651828
BB-3497, N-formyl-hydroxylamine derivativeBacteriostatic, Activity against methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus faecalis, some gram-negative bacteria.To identify novel PDF inhibitors, we screened a metalloenzyme inhibitor library and identified an N-formyl-hydroxylamine derivative, BB-3497, and a related natural hydroxamic acid antibiotic, actinonin, as potent and selective inhibitors of PDF.11158755
propargyl-linked antifolates containing a key pyridyl substituentAntibacterial activity against both methicillin-resistant S. aureus and S. pyogenes at MIC values below 0.1 ?g/mLMinimal cytotoxicity against mammalian cellsToward new therapeutics for skin and soft tissue infections: propargyl-linked antifolates are potent inhibitors of MRSA and Streptococcus pyogenes.22347365
SK&F 107647up to 1000-fold reduction in the number of E. coli recovered from bloodhematoregulatory activitiesTreatment of experimental gram-negative and gram-positive bacterial sepsis with the hematoregulatory peptide SK&F 107647.8537660
oxabicyclooctane-linked Novel bacterial topoisomerase inhibitors (NBTIs) with new tricyclic-1,5-naphthyridinone left hand side moietiesCompounds with a (R)-hydroxy-1,5-naphthyridinone moiety (7) showed potent antibacterial activity (e.g., Staphylococcus aureus MIC 0.25 ?g/mL), acceptable Gram-positive and Gram-negative spectrum with rapidly bactericidal activity.Tricyclic 1,5-naphthyridinone oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents-SAR of left-hand-side moiety25851938
TXA497, guanidinomethyl biaryl compoundsBactericidal against methicillin-resistant Staphylococcus aureus (MRSA)TXA497 as a topical antibacterial agent: comparative antistaphylococcal, skin deposition, and skin permeation studies with mupirocin25263100
Guanylated polymethacrylateskills C. albicans and S. aureus when applied to established polymicrobial biofilms.We further compared guanylated polymethacrylates with first-line antistaphylococcal and anti-Candida agents used as combinatorial therapy against polymicrobial biofilms.26490013
TXA707, FtsZ-targeting agentacts synergistically with ?-lactamsWe have developed a promising new FtsZ-targeting agent (TXA707) with potent activity against MRSA isolates resistant to current standard-of-care antibiotics.28630190
synthetic oxazolidinones, U-100592 and U-100766potent in vitro activity against Mycobacterium tuberculosisWe have prepared two potent, synthetic oxazolidinones, U-100592 and U-100766, which are currently in clinical development for the treatment of serious multidrug-resistant Gram-positive bacterial infections caused by strains of staphylococci, streptococci, and enterococci.8576909
halogenated quinoline (HQ)potent antibacterial (MIC?0.39 ?m) and biofilm eradication (MBEC 1.0-93.8 ?m) activities against drug-resistant Staphylococcus aureus, Staphylococcus epidermidis and Enterococcus faecium strains<5 % haemolysis activity against human red blood cells (RBCs) at 200 ?m and low cytotoxicity against HeLa cellsWe identified diverse analogues that are alkylated and aminated at the 2-position of the HQ scaffold and demonstrate potent antibacterial (MIC?0.39 ?m) and biofilm eradication (MBEC 1.0-93.8 ?m) activities against drug-resistant Staphylococcus aureus, Staphylococcus epidermidis and Enterococcus faecium strains while demonstrating <5 % haemolysis activity against human red blood cells (RBCs) at 200 ?m.27245927
geometrical isomers of a macrocyclic bis(bibenzyl) based on isoplagiochinThe isomer containing a 1,4-linked ring (5) showed only weak activity, whereas the isomers containing a 1,3-linked (6) or 1,2-linked (7) C ring showed potent anti-MRSA activity.We synthesized three geometrical isomers of a macrocyclic bis(bibenzyl) based on isoplagiochin, a natural product isolated from bryophytes, and evaluated their antibacterial activity towards methicillin-resistant Staphylococcus aureus (anti-MRSA activity).25999206
XRP 2868, streptograminMIC50 0.25 ?/ml, MIC90 0.5 ?/ml for pneumococci; for beta-lactamase-positive, beta-lactamase-negative, and beta-lactamase-negative ampicillin-resistant strains MIC50 is 0.25 ?/ml and an MIC90 of 1.0 ?/mlXRP 2868 showed potent activity against pneumococci and Haemophilus strains irrespective of their susceptibility to other agents.14506040