Antifungal Chemical Compounds

                                                                                                                                                                                                                                  Download data

A32390A, a new biologically active metabolite In vitro antifungal activity of A32390A was found against Candida albicans, Cryptococcus neoformans and Histoplasma capsulatum. In vitro and in vivo antifungal activity. A32390A, an isonitrile-containing derivative of mannitol, represents a new class of antifungal antibiotics.342474
Cys-reduced form of S100A7/psoriasin (redS100A7) Inhibits various filamentous fungi, including the mold Aspergillus fumigatus, but not Candida albicans Thus, selective fungal cell-penetrating Zn(2+)-chelators could be useful as an urgently needed novel antifungal therapeutic, which induces programmed cell death in numerous fungi. 26438863
FX0685, a novel triazole antifungal agentPotential antifungal for the treatment of various clinical forms of systemic candidiasis, including those caused by FLC-resistant C. albicans, as well as for the treatment of pulmonary aspergillosis In vitro and in vivo antifungal activities of FX0685, a novel triazole antifungal agent with potent activity against fluconazole-resistant Candida albicans.16010849
QACs, cationic lipo-oxazolesActivity against both fluconazole-sensitive and resistant clinical isolates of Candida albicans as well as non-albicans Candida strains. Chain-length-specific anti-Candida activity of cationic lipo-oxazoles: a new class of quaternary ammonium compounds. CONCLUSION: A novel class of QACs, called cationic lipo-oxazoles, was tested and found to exhibit anti-fungal activity against planktonic cells as well as biofilms of Candida. 29076804
1-[(biarylmethyl)methylamino]-2-(2,4-difluorophenyl)-3-(1H-1,2,4-triazol-1-yl)pro pan-2-olsBroad-spectrum antifungal activities against the most prevalent human pathogenic fungi (Candida spp. and Aspergillus fumigatus) Design, synthesis, and biological evaluation of 1-[(biarylmethyl)methylamino]-2-(2,4-difluorophenyl)-3-(1H-1,2,4-triazol-1-yl)pro pan-2-ols as potent antifungal agents: new insights into structure-activity relationships.21748853
1-R-2-([1,2,4]triazolo[1,5-c]quinazoline-2-ylthio)etanon(ol) analoguesAntibacterial and antifungal activity 1-R-2-([1,2,4]Triazolo[1,5-c]quinazoline-2-ylthio)etanon(ol)s: Synthesis, Bioluminescence Inhibition, Molecular Docking Studies, Antibacterial and Antifungal Activities. The increasing mortality due to antibacterial resistance necessitates the search for novel antimicrobial agents.27012316
2-(2'-hydroxy-5'-aminophenyl) benzoxazole (HAMBO) The inhibition provided by HAMBO was lower than that of fluconazole, showing low antifungal activity against Candida spp., but equivalent to that of benzoxazoles tested in similar studies.: HAMBO showed fungistatic activity against all analysed strains. In vitro antifungal activity of 2-(2'-hydroxy-5'-aminophenyl)benzoxazole in Candida spp. Strains. This class of novel benzoxazole compounds may be used as template to produce better antifungal drugs. 19302462
2,3,5-tri-O-benzyl-d-ribose (compound 1) and a 2,5-functionalized imidazole (compound 2Inhibited chitin synthases in vitro with IC50 values of 1.8 and 10 microM, respectively and antifungal activity against B. cinerea BD90 strain with MIC values of 190 and 100 microM, respectively Discovery of two new inhibitors of Botrytis cinerea chitin synthase by a chemical library screening. Chitin synthases polymerize UDP-GlcNAC to form chitin polymer, a key component of fungal cell wall biosynthesis.23886809
2,5-disubstituted tetrazole derivatives containing benzothiazole, benzoxazole or phenylsulfonyl moiety synthesized by N-alkylation of aryltetrazole with 2-[(3-chloropropyl)sulfanyl]-1,3-benzothiazole or 2-[(3-chloropropyl)sulfanyl]-1,3-benzoxazole and Michael-type addition of aryltetrazole to phenyl vinyl sulfone All the tetrazole derivatives acted at the same level against C. albicans and demonstrated a high cell growth inhibition (97-99%) at the concentrations ranging from 16 to 0.0313 microg/mLSynthesis of novel tetrazole derivatives and evaluation of their antifungal activity. In this context new 2,5-disubstituted tetrazole derivatives containing benzothiazole, benzoxazole or phenylsulfonyl moiety were synthesized by N-alkylation of aryltetrazole with 2-[(3-chloropropyl)sulfanyl]-1,3-benzothiazole or 2-[(3-chloropropyl)sulfanyl]-1,3-benzoxazole and Michael-type addition of aryltetrazole to phenyl vinyl sulfone.27745991
2-Aminonicotinamide DerivativesOverall MIC80?between 0.0313 to 4.0 microg mL-1, compounds 11 g [2-amino-N-((5-(((2-fluorophenyl)amino)methyl)thiophen-2-yl)methyl)nicotinamide] and 11 h [2-amino-N-((5-(((3-fluorophenyl)amino)methyl)thiophen-2-yl)methyl)nicotinamide] displayed excellent activity against C. albicans, with MIC80?values of 0.0313 ?g mL-1Synthesis and Biological Evaluation of Novel 2-Aminonicotinamide Derivatives as Antifungal Agents.28071858
2-cyclohexylidenhydrazo-4-phenyl-thiazole 99.9% loss of C. albicans viability, also active in inhibiting the growth of C. albicans ATCC 10231 biofilms CONCLUSIONS: Based on these results, EM-01D2 could represent a template for the development of novel fungicidal agents. 15772140
2'-hydroxy-4'-methoxychalconeActivity against fluconazole-resistant Candida albicansTo identify effective and low toxicity synergistic antifungal compounds, 24 derivatives of chalcone were synthesized to restore the effectiveness of fluconazole against fluconazole-resistant Candida albicans. Of the synthesized compounds, 2'-hydroxy-4'-methoxychalcone (8) exhibited the most potent in vitro (FICI=0.007) effects.27210436
3-(halogenated phenyl)-5-acyloxymethyl- 2,5-dihydrofuran-2-one derivativesThe furanone derivatives displayed broad-spectrum in vitro activity against potentially pathogenic yeasts and molds, especially Aspergillus spp. (MIC Thus, the halogenated 3-phenyl-5-acyloxymethyl derivatives of 2,5-dihydrofuran-2-one represent a novel, promising group of compounds with significant activity against relevant opportunistic fungi that are pathogenic to humans. 14982778
3-Aryl-4-[alpha-(1H-imidazol-1-yl)arylmethyl]pyrrole derivativesThe most active derivative (27) was twice as potent (MIC90) as bifonazole, and its activity was 4 times greater than those of miconazole and ketoconazole.: The other nine compounds showed antifungal activity of the same order of that of bifonazole and were ca. 2 times as active as miconazole and ketoconazole.A new class of potent antifungal agents, namely, 3-aryl-4-[alpha-(1H-imidazol-1-yl)arylmethyl]-pyrroles, is described.7473549
4-(5, 6-dichloro-1H-benzimidazol-2-yl)-N-substituted benzamide derivativesAntibacterial and Antifungal (Candida albicans) activity Synthesis and potent antimicrobial activity of some novel 4-(5, 6-dichloro-1H-benzimidazol-2-yl)-N-substituted benzamides. A series of 4-(5, 6-dichloro-1H-benzimidazol-2-yl)-N-substituted benzamides were synthesized and evaluated for antibacterial and antifungal activities against Staphylococcus aureus, methicillin-resistant S. aureus (MRSA), methicillin-resistant S. epidermis (MRSE), Enterococcus faecalis, Escherichia coli and Candida albicans.15476288
4-bromo-5Z-(bromomethylene)-3-butylfuran-2-one (BF1)Inhibition of Candida albicans growth In this study, we demonstrate the antifungal activity of brominated furanones on C. albicans. Studying the structure and activity of this class of furanones reveals that the exocyclic vinyl bromide conjugated with the carbonyl group is the most important structural element for fungal inhibition.19756586
A series of 3,4-dichloro-, 3-methyl and non-substituted maleimidesOf the 63 compounds evaluated, 25 compounds had interesting inhibitory potency with EC50 < 10 microg mL(-1). N-(3,5-Dichlorophenyl)-3,4-dichloromaleimide (EC50 = 1.11 microg mL(-1)) and N-octyl-3-methylmaleimide (EC50 = 1.01 microg mL(-1)) were more potent than the commercial fungicide dicloran (EC50 = 1.72 microg mL(-1)). CONCLUSION: The present work demonstrates that some maleimides can be used as potential lead compounds for developing novel antifungal agents against S. sclerotiorum. 24796632
Acetophenone-derived bis Mannich bases, B1-B5, bis(beta-aroylethyl)methylamine hydrochloridesAll compounds studied have shown antifungal activity, especially against dermatophytes (Trichophyton rubrum, Trichophyton mentagrophytes, Trichophyton tonsurans, and Microsporum canis), in the concentration range studied (2-128 microng/ml) Antifungal evaluation of bis Mannich bases derived from acetophenones and their corresponding piperidinols and stability studies. The development of resistance to current antifungal therapeutics drives the search for effective new agents.12392084
Aflastatin ACompletely inhibited aflatoxin production by Aspergillus parasiticus NRRL 2999 in liquid medium or on agar plate at a concentration of 0.5 microgram/ml Aflastatin A, a novel inhibitor of aflatoxin production by aflatoxigenic fungi. Aflastatin A, a novel inhibitor of the production of aflatoxin by aflatoxigenic fungi, has been isolated from the solvent extract of mycelial cake of Streptomyces sp. and its molecular formula was determined as C62H115NO24.9099219
Alkylated mono-, bis-, and trisbenzimidazole derivativesMIC values ranging from 15.6 to 0.975 microg/mLSynthesis and investigation of novel benzimidazole derivatives as antifungal agents. 27301676
Ambroxol Hydrochloride Combined with FluconazoleAmbroxol hydrochloride (128 ?g/mL) exhibits synergistic antifungal effects in combination with fluconazole (2 ?g/mL) against resistant planktonic?Candida albicans?(C. albicans) cells and resistant C. albicans biofilms In this study, we found that ambroxol hydrochloride (128 ?g/mL) exhibits synergistic antifungal effects in combination with fluconazole (2 ?g/mL) against resistant planktonic Candida albicans (C. albicans) cells. The results show the potential role for this drug combination as a therapeutic alternative to treat resistant C. albicans and provide insights into the development of antifungal targets and new antifungal agents. 28439502
Aminoglycoside antibiotics combined with different sulphate-transport inhibitorsCombinations decreased the respective MICs by greater than 8-fold, active aginst human pathogens Candida albicans, C. glabrata and Cryptococcus neoformans, the food spoilage organism Zygosaccharomyces bailii and the phytopathogens Rhizoctonia solani and Zymoseptoria tritici.Novel, Synergistic Antifungal Combinations that Target Translation Fidelity26573415
Anthracene-9-carboxylic and niflumic acidEffect on growth, energy metabolism and anionic current of mycelium of fungus Phycomyces blakesleeanus Growth inhibition of fungus Phycomyces blakesleeanus by anion channel inhibitors anthracene-9-carboxylic and niflumic acid attained through decrease in cellular respiration and energy metabolites. Increasing resistance of fungal strains to known fungicides has prompted identification of new candidates for fungicides among substances previously used for other purposes.28100310
AR-12, Celecoxib DerivativeActivity against yeasts (e.g., Candida albicans, non-albicans Candida spp., Cryptococcus neoformans), molds (e.g., Fusarium, Mucor), and dimorphic fungi (Blastomyces, Histoplasma, and Coccidioides) with MICs of 2 to 4 ?g/ml. The Celecoxib Derivative AR-12 Has Broad-Spectrum Antifungal Activity In Vitro and Improves the Activity of Fluconazole in a Murine Model of Cryptococcosis.27645246
Aryl isonitrile compoundsBroad-spectrum antifungal activity primarily against species of Candida and Cryptococcus, most potent derivatives are capable of inhibiting growth of these key pathogens at concentrations as low as 0.5 microMThe most active compounds exhibit an excellent safety profile and are non-toxic to mammalian cells even at concentrations up to 256 microM Investigation of aryl isonitrile compounds with potent, broad-spectrum antifungal activity. 28385596
aryl-1,2,4-triazol-3-ylthio analogues of fluconazole (ATTAF-1 and ATTAF-2)Showed lowest geometric mean MICs, combinations fluconazole exhibited synergistic effects against fluconazole-susceptible (22 of 23 isolates), fluconazole-susceptible dose-dependent (10 of 13 isolates), and fluconazole-resistant (1 of 16 isolates) Candida isolates. In Vitro Activities of Novel Azole Compounds ATTAF-1 and ATTAF-2 against Fluconazole-Susceptible and -Resistant Isolates of Candida Species. The in vitro activities of two novel azole compounds (aryl-1,2,4-triazol-3-ylthio analogues of fluconazole [ATTAFs]) and five comparator antifungal agents against 52 clinical Candida isolates from 5 different species were determined.27795371
ASP2397ASP2397 MIC50 values were 0.5 mg/L (0.25 to 1) and 0.25 mg/L(0.06 to 0.25) against A. fumigatus CYP51A wild-type isolates and were similarly 0.5 mg/L (0.125 to >4) and 0.125 mg/L (0.06 to >4) against azole-resistant A. fumigatus isolates, respectively. ASP2397 was active against A. terreus CYP51A wild-type isolates (MIC 0.5 to 1) In Vitro Activity of ASP2397 against Aspergillus Isolates with or without Acquired Azole Resistance Mechanisms. ASP2397 is a new compound with a novel and as-yet-unknown target different from that of licensed antifungal agents.26552973
AzoxybacilinBroad spectrum antifungal activity, especially active against mycelial fung A new methionine antagonist that has antifungal activity: mode of action. A new antifungal, azoxybacilin (an unusual amino acid with an azoxy moiety) was identified from Bacillus cereus, and its in vitro antifungal activity and mode of action were investigated.7928678
Benzimidazole derivatives [(S)-2-aminoalkyl benzimidazole derivative, (S)-2-(1-Aminoisobutyl)-1-(3-chlorobenzyl) benzimidazole](S)-2-(1-Aminoisobutyl)-1-(3-chlorobenzyl) benzimidazole showed the highest antifungal activity against a number of clinical isolates of several species of pathogenic Candida yeasts.(S)-2-(1-Aminoisobutyl)-1-(3-chlorobenzyl) benzimidazole showed the showed best compatibility with human cells in several cell culture modelsA screening assay based on host-pathogen interaction models identifies a set of novel antifungal benzimidazole derivatives.21746957
Benzofuran derivativesAntifungal activity against C. albicans Synthesis and biological activities of benzofuran antifungal agents targeting fungal N-myristoyltransferase. The C-4 side chain modification of lead compound 1 has resulted in the identification of a potent and selective Candida albicans N-myristoyltransferase (CaNmt) inhibitor RO-09-4609, which exhibits antifungal activity against C. albicans in vitro.13129583
Berberine derivative B-7b and fluconazole The potent synergistic activity of B-7b in combination with FLC against FLC-resistant C. albicans, the disruption of protein folding and processing and the weakening of cells' self-defensive ability contributed to the synergism of FLC and B-7b. Together, these results suggested novel scaffold BBR derivative B-7b could be a promising synergist in combination with FLC for the treatment of invasive fungal infections. 25992630
bis(N-amidinohydrazones) and N-(amidino)-N'-aryl-bishydrazonesAntibacterial and antifungal agents, MIC values ranging from (less than) 0.5 to (greater tahn) 500 microM against bacteria and 1.0 to (greater than) 31.3 micro g/mL against fungiMinimal emergence of drug resistance to these newly synthesized compounds by bacteria and fungi even after 15 passages, and we found weak to moderate inhibition of the human Ether-?-go-go-related gene (hERG) channel with acceptable IC50?values ranging from 1.12 to 3.29 microM Overall, these studies show that bis(N-amidinohydrazones) and N-(amidino)-N'-aryl-bishydrazones are potentially promising scaffolds for the discovery of novel antibacterial and antifungal agents. 27769670
BromoquinolActive against Aspergillus fumigatusThe quinoline bromoquinol exhibits broad-spectrum antifungal activity and induces oxidative stress and apoptosis in Aspergillus fumigatus. The most potent, bromoquinol, shows potent wide-spectrum antifungal activity that was blocked in the presence of exogenous iron.28475687
CAN-296, complex carbohydrateInhibited proton pumping of Candida albicans, Candida glabrata, Candida krusei, Candida guilliermondii and Saccharomyces cerevisiae at low concentrations (0.078-1.25 mg/l) Proton translocating ATPase mediated fungicidal activity of a novel complex carbohydrate: CAN-296. CAN-296 is a complex carbohydrate (approximately 4300 Da) isolated from the cell wall of Mucor rouxii.10755243
Combination therapies using L-743,872, a pneumocandin antifungal drug, and amphotericin B or fluconazoleShowed additive and autonomous activities against fluconazole-resistant isolates The results of this study suggest that L-743,872 can enhance the efficacy of fluconazole or amphotericin B in vitro and indicate a potential role for L-743,872 in combination therapy against C. neoformans. 9021188
Combination therapy of bafilomycin A(1), fluconazole, and the pneumocandin MK-0991/caspofungin acetate (L-743,873) with calcineurin inhibitors FK506 and L-685,818Activity against Cryptococcus neoformansSynergistic antifungal activities of bafilomycin A(1), fluconazole, and the pneumocandin MK-0991/caspofungin acetate (L-743,873) with calcineurin inhibitors FK506 and L-685,818 against Cryptococcus neoformans10681348
Combination therapy of lysine and amphotericin B Lysine enhances the effect of AmB against Candida albicans in vitro Using AmB together with lysine may be a promising strategy for the therapy of disseminated candidiasis. 26711896
Copper(II) complexes of 2-methylthionicotinate (2-MeSNic) of the composition Cu(2-MeSNic)2(MeNia)(2).4H2O (where MeNia is N-methylnicotinamide), and Cu(2-MeSNic)2(Nia)(2).2H2O (where Nia is nicotinamide) and Cu(2-MeSNic)2L2 (where L is isonicotinamide, iNia, or ethyl nicotinate, EtNic)IC50 1.5-2.3 mmol/L against Rhizopus oryzae and Microsporum gypseum, adducts with Nia, MeNia and EtNic at 5 mmol/L induced morphological changes in growing hyphae of Botrytis cinerea, inhibition of sporulation (> 90%) of Alternaria alternata by Cu(2-MeSNic)2.H2OAntifungal activity of new copper(II) complexes of 2-methylthionicotinate (2-MeSNic) of the composition Cu(2-MeSNic)2(MeNia)(2).4H2O (where MeNia is N-methylnicotinamide), and Cu(2-MeSNic)2(Nia)(2).2H2O (where Nia is nicotinamide) and Cu(2-MeSNic)2L2 (where L is isonicotinamide, iNia, or ethyl nicotinate, EtNic) were tested on various strains of filamentous fungi by the macrodilution method.12094729
CS-758, a novel triazoleCS-758 exhibited potent in vitro activity (MICs, 0.004 to 0.06 micro g/ml) against the strains used in this murine model including fluconazole-susceptible dose-dependent and fluconazole-resistant strains (fluconazole MICs, 16 to 64 micro g/ml) Efficacy of CS-758, a novel triazole, against experimental fluconazole-resistant oropharyngeal candidiasis in mice. The therapeutic efficacy of CS-758, a novel triazole, was evaluated against experimental murine oropharyngeal candidiasis induced by Candida albicans with various susceptibilities to fluconazole.12543666
CW-8/haemofunginInhibits the growth of pathogenic Aspergillus, Candida, Fusarium and Rhizopus isolates at micromolar concentrationsOnly weakly affect the growth of mammalian cell lines Identification and characterization of haemofungin, a novel antifungal compound that inhibits the final step of haem biosynthesis.26747101
Cyclohexyliden- and 2-methylcyclohexyliden-hydrazo-4-arylthiazolesFive out of nine compounds were active towards Candida albicans 25 FLC resistant isolated from clinical specimens On the basis of our data we can conclude that these derivatives are promising agents for the treatment of resistant C. albicans. 26745285
Cyclosporine (CsA) derivatives, (gamma-OH) MeLeu(4)-Cs (211-810) and D-Sar (alpha-SMe)(3) Val(2)-DH-Cs (209-825) Our findings identify calcineurin as a novel antifungal drug target and suggest nonimmunosuppressive CsA analogs warrant investigation as antifungal agents. 10602736
Cystatin, affinity-purified from chicken egg white (CEWC) CEWC inhibited the growth of azole-sensitive Candida albicans isolates with minimal inhibitory concentration (MIC) values ranging from 0.8 to 3.3 micromol l(-1), a potency comparable with those of fluconazole and histatin 5, the antimicrobial peptide of the human saliva.The antifungal properties of chicken egg cystatin against Candida yeast isolates showing different levels of azole resistance. The increasing incidence of fungal infections together with the emergence of strains resistant to currently available antifungal drugs calls for the development of new classes of antimycotics.19549107
D0870, antifungal triazoleMICs for 50 and 90% of the isolates tested were < or = 0.0078 and 0.06 micrograms/ml In vitro activity of a new antifungal triazole, D0870, against Candida albicans isolates from oral cavities of patients infected with human immunodeficiency virus. We investigated the in vitro activity of a new antifungal triazole, D0870, against 100 Candida albicans isolates from the oral cavities of patients infected with human immunodeficiency virus by using a broth macrodilution method following the recommendations provided by the National Committee for Clinical Laboratory Standards (document M27-P).7872746
D75-4590Potent activities against various Candida species, specific inhibitor of beta-1,6-glucan synthesis These lines of evidence indicate that D75-4590 is a promising lead compound for novel antifungal drugs.19015325
Derivatives of the ring system indolo[1,2-c]benzo[1,2,3]triazine 5 synthesized by diazotization of substituted 2-(2-aminophenyl)indolesAntitumour and antifungal activityAntifungal activity at concentrations very close to those inhibiting the proliferation of human cells Derivatives of the new ring system indolo[1,2-c]benzo[1,2,3]triazine with potent antitumor and antimicrobial activity. Derivatives of the new ring system indolo[1,2-c]benzo[1,2,3]triazine 5 were synthesized by diazotization of substituted 2-(2-aminophenyl)indoles followed by an intramolecular coupling reaction of the diazonium group with the indole nitrogen.10411476
Dichloromethyl-4-chloro-3-nitrophenylsulfone (Compound 1) and chlorodibromomethyl-4-hydrazino-3-nitrophenylsulfone (Compound 2Compound 1 showed higher activity (% = 100 at 4 ?g/ml) than Compound 2 (MIC90 = 16 ?g/ml) against Candida sppSulfone derivatives reduce growth, adhesion and aspartic protease SAP2 gene expression. Fungal virulence factors represent a strategy for the design of new compounds with effective activities against Candida spp.24880247
Diguanidino 1-methyl-2,5-diaryl-1H-pyrroles The antifungal activities evaluated against Candida spp. and Aspergillus spp. Synthesis of some diguanidino 1-methyl-2,5-diaryl-1H-pyrroles as antifungal agents. A series of novel 2,5-bis(guanidino-aryl)-1-methyl-1H-pyrroles 9a-h has been synthesized starting from 1-methyl-1H-pyrrole.15978808
Eugenol and methyl eugenolAntifungal activity by targeting sterol biosynthesis, additional methyl group to eugenol increases its antifungal activity The observed fungicidal characteristics of both eugenol and methyl eugenol indicate that both the compounds might be promising antifungal agents defining a new class of antimycotics. 19835945
F901318A. fumigatus WT, MIC90 0.125 mg/L (range 0.031-0.125); TR34/L98H,TR46/Y121F/T289A and azole resistant without known resistance mechanisms, MIC90 0.125 mg/L (range 0.031-0.25); A. fumigatus with cyp51A-associated point mutations, MIC90 0.062 mg/L (range 0.015-0.125); and other species, A. calidoustus MIC90 0.5 mg/L (range 0.125-0.5), A. flavus MIC90 0.062 mg/L (range 0.015-0.62), A. nidulans MIC90 0.125 mg/L (range 0.062-0.25) and A. tubingensis MIC90 0.062 mg/L (range 0.015-0.25) In vitro activity of the novel antifungal compound F901318 against difficult-to-treat Aspergillus isolates.28605488
FK463, a (1,3)-beta-D-glucan synthase inhibitorEfficacy against azole-resistant Candida albicans Efficacy of FK463, a (1,3)-beta-D-glucan synthase inhibitor, in disseminated azole-resistant candida albicans infection in mice. The efficacy of FK463, a new (1,3)-beta-D-glucan synthase inhibitor, against azole-resistant Candida albicans strains has been studied. In our study, FK463 was found to be a potent antifungal agent against disseminated infection with azole-resistant C. albicans.10817741
FK-506, immunosuppressant agentantagonist of T-cell activation and an inhibitor of fungal growth Antifungal properties of the immunosuppressant FK-506: identification of an FK-506-responsive yeast gene distinct from FKB1.1715022
GlabridinSignificant decrease in MICs against fluconazole-resistant C. glabrata (MIC50: 8 micro g/mL) Glabridin is an originally natural substrate with multiple biological activities which propose it as a novel anticancer, antimicrobial and antifungal agent.28595940
Glucosylated solasodine-3-O-beta-d-glucopyranoside?Activity against wild type Candida albicans Our study reveals that glucosylation is an alternative approach for introducing potential antifungal activity into C.?albicans cells and overcoming the drug-resistance resulting from hyperactivation of efflux pumps. 28919409
Guanylated polymethacrylatesThe most potent compound kills 99.98% of S. aureus and 82.2% of C. albicans at a concentration of 128 mg/LSearching for new strategies against polymicrobial biofilm infections: guanylated polymethacrylates kill mixed fungal/bacterial biofilms. OBJECTIVES: Biofilm-related human infections have high mortality rates due to drug resistance.26490013
Halogenated quinoline (HQ) analoguesFour HQ analogues inhibited C. albicans growth with a minimum inhibitory concentration (MIC) of 100 nM, whilst 16 analogues effectively inhibited C. neoformans at MICs of 50-780 nM. Remarkably, two HQ analogues eradicated mature C. albicans and C. neoformans biofilms [minimum biofilm eradication concentration (MBEC) = 6.25-62.5 microM]. HQs are a promising class of small molecules that may be useful in future antifungal treatments. 27256584
Hydrogen peroxideAdjunctive therapy for treatment of mucormycosis Adjunctive therapy with hydrogen peroxide. Mucormycosis is a devastating fungal disease affecting mainly diabetic and immunosuppressed patients and frequently causing death.8810881
HydroxyaldiminesActivity against Cryptococcus gattii and Cryptococcus neoformans strains The in vitro anticryptococcal activity of hydroxyaldimines against various strains of C.?gattii and C.?neoformans indicates the potential of this class of molecules as lead compound for the development of selective and efficient anticryptococcal agents.23594040
IB-367Exerted a fungicidal activity against Trichophyton mentagrophytes, T. rubrum and Microsporum canis We propose IB-367 as a promising candidate for the future design of antifungal drugs. 26058322
Imidazolium salt 1-n-hexadecyl-3-methylimidazolium chloride (C16 MImCl)Prevents, in concentrations as low as 0?028 microg ml(-1) , the biofilm formation of multidrug-resistant Candida tropicalis isolates As such, C16 MImCl has been identified as a promising antimicotic pharmaceutical candidate for the treatment of candidiasis infections25294047
Imidazolium salts (1-n-Hexadecyl-3-methylimidazolium chloride (C16 MImCl) and 1-n-hexadecyl-3-methylimidazolium methanesulfonate (C16 MImMeS)) All dermatophytes were inhibited by IMS, where the lowest minimum inhibitory concentration (MIC) values were observed for salts with n-hexadecyl segment in the cation side chain, containing either the chloride or methanesulfonate anion. 1-n-Hexadecyl-3-methylimidazolium chloride (C16 MImCl) and 1-n-hexadecyl-3-methylimidazolium methanesulfonate (C16 MImMeS) acted as fungicides, even in extremely low concentrations, wherein C16 MImMeS exerted this effect on 100% of the tested dermatophytes. The expressive antifungal activity of IMS, combined with the in vitro nontoxicity, makes them promising compounds for the safe and effective treatment of dermatophytoses, mainly when this skin mycosis is unresponsive to conventional drugs. 26043668
JS399-19, cyanoacrylate fungicideTargets the motor domain of type I myosin, specific to FusariumReal-time imaging was used to study the effects of a novel Fusarium-specific cyanoacrylate fungicide (JS399-19) on growth and morphology of four Fusarium sp. This fungicide targets the motor domain of type I myosin.27914536
KB425796-A congenersCongeners of KB425796-A, named KB425796-B, -C, -D, -E, -F, -G, -H, -I, -J and -K, which exhibited diverse antifungal potencies against A. fumigatusIdentification of ten KB425796-A congeners from Paenibacillus sp. 530603 using an antifungal assay against Aspergillus fumigatus in combination with micafungin. 23778114
KB425796-C in combination with micafunginAntifungal activity against micafungin-resistant fungi and was fungicidal to Trichosporon asahii in vitro Synergistic antifungal activity of KB425796-C in combination with micafungin against Aspergillus fumigatus and its efficacy in murine infection models. KB425796-C is a novel antifungal metabolite produced by the newly isolated bacterial strain Paenibacillus sp.23756682
KP-363, butenafine hydrochlorideWide spectrum activity in vitro against particularly dermatophytes (87 strains; minimal inhibitory concentration (MIC) range, 0.0015 to 0.05 microgram/ml), and also against Aspergillus (15 strains; MIC range, 0.025 to 0.78 microgram/ml), Cryptococcus neoformans (4 strains; MICs 0.78 and 1.56 micrograms/ml) and yeasts of genus Candida (67 strains; MIC range, 3.13 to greater than 100 micrograms/ml). [Synthesis and antifungal activity of butenafine hydrochloride (KP-363), a new benzylamine antifungal agent]. In screening of new antifungal agents, bis(naphthalenemethyl)amines were found to have more potent antifungal activity than clotrimazole.2056447
L-733,560, pneumocandin antifungal agentThe mean MICs of L-733,560 were 0.15 microgram/ml for C. lusitaniae, 0.72 microgram/ml for C. parapsilosis, 0.78 micrograms/ml for C. krusei, and 1.25 micrograms/ml for C. guilliermondii The results indicate that the new antifungal agent L-733,560 demonstrated the best activity with the lowest MICs against C. albicans, T. glabrata, C. tropicalis, and C. kefyr, less activity against C. krusei, C. lusitaniae, and C. parapsilosis, and the least activity against C. guilliermondii.8593003
L-733560, a new water-soluble hybrid of L-705589 and L-731373 Growth inhibition kinetic studies against Candida albicans revealed fungicidal activity within 3 to 5 h In vitro evaluation of the pneumocandin antifungal agent L-733560, a new water-soluble hybrid of L-705589 and L-731373.7625791
Luliconazole, Lanoconazole, and EfinaconazoleActivity against Melanized Fungi and Relatives Therefore, it appears that these new imidazole and triazole drugs are promising candidates for the treatment of infections due to melanized fungi and their relatives. Copyright ? 2017 American Society for Microbiology. DOI: 10.1128/AAC.00635-17 PMCID: PMC565504928848012
Macrocyclic amidinoureasPotent antifungal activity against Candida spp Biological Characterization and in Vivo Assessment of the Activity of a New Synthetic Macrocyclic Antifungal Compound. We recently identified a novel family of macrocyclic amidinoureas showing potent antifungal activity against Candida spp.27045868
MagnololMIC?ranging from 10 to 40 micro g/mL against C. albicans?and non-albicans?Candida?species, especially fluconazole-resistant?Candida krusei, with the minimum inhibitory concentrations , BMIC90?(minimum concentration with 90%?Candida?biofilm inhibited) values of magnolol ranged from 20 to 160 micro g/mL As an alternative and broad-spectrum antifungal agent, magnolol might be of benefit to the treatment of refractory Candida infection. 28919715
ME1111MIC90 against dermatophyte strains was 0.25 micro g/ml, MFC90s against Trichophyton rubrum and Trichophyton mentagrophytes were 8 micro g/mlIn vitro antifungal activity of ME1111, a new topical agent for onychomycosis, against clinical isolates of dermatophytes. ME1111 is a novel selective inhibitor of succinate dehydrogenase (complex II) of dermatophyte species, whose small molecular weight enhances its ability to penetrate the nail plate.26055386
ME1111ME1111 strongly inhibited the succinate-2,6-dichlorophenolindophenol reductase reaction in Trichophyton rubrum and T. mentagrophytes (50% inhibitory concentrations [IC50s] of 0.029 and 0.025 microg/ml, respectively) ME1111 is a novel antifungal agent that is active against dermatophytes, has an excellent ability to penetrate human nails, and is being developed as a topical agent for onychomycosis.26596944
ME1401, a new antifungal agentBroad antifungal spectrum and inhibited all of the 428 strains of 52 species of pathogenic yeasts and filamentous fungi tested at concentrations ranging from 0.01 to 12.5 micrograms/ml. In vitro activity of ME1401, a new antifungal agent. Yamaguchi H, Uchida K, Hiratani T, Hara T, Fukuyasu H, Kazuno Y, Inouye S. The in vitro antifungal activity of ME1401, a potential topical antifungal agent, was compared with that of haloprogin, clotrimazole, miconazole, tolnaftate, and ciclopirox olamine by using an agar dilution procedure.3800346
Mono, bis and quaternary Mannich bases derived from acetophenoneActivity against Saccharomyces cerevisiae Antifungal activity of some mono, bis and quaternary Mannich bases derived from acetophenone. The development of resistance to current antifungal therapeutics drives search for new effective agents.11215330
N-(1-benzyl-2-phenylethylidene)-N'-[4-(aryl)thiazol-2-yl]hydrazone (1a-e) and N-(1-phenylbutylidene)-N'-[4-(aryl)thiazol-2-yl]hydrazone (2a-e) derivativesAntifungal activities tested against Candida albicans, Candida glabrata, Candida utilis, Candida tropicalis, Candida krusei, Candida zeylanoides, and Candida parapsilosis Studies on hydrazone derivatives as antifungal agents. The increasing clinical importance of drug-resistant fungal pathogens has urged additional need to fungal research and new antifungal compound development.18665994
Naphthoquinone thiol-crown ether analoguesBis-naphthoquinone thiol-crown ether 7a was the most potent inhibitor against Staphylococcus aureus methicillin resistance with MIC value of 2.68 microM. Efficient synthesis of 'redox-switched' naphthoquinone thiol-crown ethers and their biological activity evaluation.11937353
NC1175, styryl ketoneAll 20 clinical isolates of A. fumigatus examined were susceptible to NC1175 (MIC = 5.54 +/- 2.48 mg/L; range 2.92-11.68 mg/L), and the minimum lethal concentration (MLC) was only twice the MIC, suggesting that NC1175 is fungicidal In-vitro and in-vivo susceptibility of Aspergillus fumigatus to a novel conjugated styryl ketone. We investigated the in-vitro and in-vivo susceptibility of Aspergillus fumigatus to the novel conjugated styryl ketone NC1175 and the results were compared with those obtained for amphotericin B and itraconazole.9848441
NCK-10, Aryl-alkyl-lysinesInhibits growth Candida spp., Cryptococcus spp., and Aspergillus fumigatus, mechanism is disruption of the fungal cell membrane Overall, aryl-alkyl-lysines were found to be excellent compounds that warrant further investigation as novel antifungal agents. 28238268
N-dimethylaminoacetyl-partricin A 2-dimethylaminoethylamide diaspartate (SPA)Showed in vivo activity enhancing mouse resistance to cryptococcal meningoencephalitis and in vitro by potentiating the anticryptococcal activity of murine microglial cells Potent antifungal effects of a new derivative of partricin A in a murine model of cerebral cryptococcosis.9056019
New heptaketides, biatriosporins A-L (1-12), biatriosporin M (13) (a ramulosin derivative), and 19 known compounds (14-32)The most potent compound, compound 4, also sensitized clinically derived azole-resistant Candida albicans strains to fluconazole (FLC)Heptaketides from an Endolichenic Fungus Biatriospora sp. and Their Antifungal Activity27556953
New series of thiazolyl-triazole Schiff bases B1-B15Potential anti-Candida activity with Compound B10 being more potent New Thiazolyl-triazole Schiff Bases: Synthesis and Evaluation of the Anti-Candida Potential. In the context of the dangerous phenomenon of fungal resistance to the available therapies, we present here the chemical synthesis of a new series of thiazolyl-triazole Schiff bases B1-B15, which were in vitro assessed for their anti-Candida potential.27879678
New sulfated sterols, geodisterol-3-O-sulfite (1) and 29-demethylgeodisterol-3-O-sulfite (2)Combat the resistance associated with opportunistic fungal infections caused by C. albicans Reversal of fluconazole resistance by sulfated sterols from the marine sponge Topsentia sp.19653640
Nitric-oxide releasing aspirin (NO-ASA) Adhesion to abiotic surfaces, a critical event for biofilm formation, was evaluated in 96-well polystyrene plates using crystal violet assay; 125 micro M NO-ASA significantly inhibited C. albicans adhesion. NO-ASA is a promising novel antibiofilm agent for treating fluconazole-resistant strains of C. albicans. 28493889
NND-502, imidazole compound The geometric mean (GM)-MICs of NND-502 for 25 strains of M. furfur, 15 strains of M. sympodialis and ten strains of M. slooffiae were approximately 1.4, 0.1 and 1.0 mg/l, respectively In vitro activity of novel imidazole antifungal agent NND-502 against Malassezia species.12636984
Novel Schiff base [hetero-dinuclear copper(II) Mn(II) complex] (SB) derivativeActivity against Candida albicans In the current study, a novel Schiff base [hetero-dinuclear copper(II) Mn(II) complex] (SB) derivative was investigated for its anticandidal activity against Candida albicans and possible mechanisms inducing cell death.29080032
N-substituted phthalimides (N-vinylphthalimide (4) and 8-[4-(phthalimide-2-yl) butyloxy] quinoline (13) )Compound (4) and (13) were identified as the most promising candidates against B. cinerea and A. solani with the IC50 values of 7.92 microg/mL and 10.85 microg/mL respectively.? N-vinylphthalimide (4) and 8-[4-(phthalimide-2-yl) butyloxy] quinoline (13) were identified as the most promising candidates against B.?cinerea and A.?solani with the IC50 values of 7.92??g/mL and 10.85??g/mL respectively.27079471
Nylon-3 polymers This polymer is active on its own and in synergy with existing antifungal drugs against multiple species of Candida and Cryptococcus, acts synergistically with azoles against different species of Aspergillus, including some azole-resistant strains.Displayi only mild to moderate toxicity toward mammalian cells.: These findings indicate that nylon-3 polymers are a promising lead for development of new antifungal therapeutic strategies. Copyright ? 2017 American Society for Microbiology.28739790
Orally absorbable imidazole derivatives: BAY n 7133 and BAY 1 9139Activity comparable to those of ketoconazole and miconazole In-vitro inhibitory activities of 2 new orally absorbable imidazole derivatives: BAY n 7133 and BAY 1 9139.6314564
Pathogen Box chemical library (Medicines for Malaria Venture [MMV], Switzerland) (MMV688768, MMV687273, and MMV687807The most potent compound MMV688768, displayed increased antibiofilm activity compared to its activity against planktonic cultures, indicating that it may affect processes with a predominant role during the biofilm mode of growth, in vitro combination assays showed a synergistic interaction between compound MMV688768 and fluconazole against preformed biofilms. Interestingly, the most potent of these, compound MMV688768, displayed increased antibiofilm activity compared to its activity against planktonic cultures, indicating that it may affect processes with a predominant role during the biofilm mode of growth.27795383
PcPAF, antifungal protein produced by the fungal strain Penicillium citrinum W1PcPAF displayed antifungal activity against Trichoderma viride, Fusarium oxysporum, Paecilomyces variotii, and Alternaria longipes at minimum inhibitory concentrations of 1.52, 6.08, 3.04, and 6.08 micro g/disc, respectively.Purification and identification of a novel antifungal protein secreted by Penicillium citrinum from the Southwest Indian Ocean. The results suggested that PcPAF may represent a novel antifungal protein with potential application in controlling plant pathogenic fungal infection. 24931500
PLD-118Inhibitor of candida isoleucyl-tRNA synthetase in fluconazole (FLC)-resistant Candida albicans Efficacy of PLD-118, a novel inhibitor of candida isoleucyl-tRNA synthetase, against experimental oropharyngeal and esophageal candidiasis caused by fluconazole-resistant C. albicans. PLD-118, formerly BAY 10-8888, is a synthetic antifungal derivative of the naturally occurring beta-amino acid cispentacin.15388459
Pneumocandins L-733,560 and L-743,872Activity against amphotericin B- and fluconazole-resistant Candida isolates In vitro growth-inhibitory activity of pneumocandins L-733,560 and L-743,872 against putatively amphotericin B- and fluconazole-resistant Candida isolates: influence of assay conditions. L-733,560 and L-743,872 are water-soluble pneumocandins with potent antifungal activity.9292427
R-135853, a sordarin derivativeR-135853 also exhibited potent activities against fluconazole-susceptible dose-dependent and fluconazole-resistant strains of C. albicans, with MICs ranging from 0.03 to 0.06 micro g/mlAntifungal activities of R-135853, a sordarin derivative, in experimental candidiasis in mice. R-135853 exhibited potent in vitro activities against Candida albicans (fluconazole-susceptible strains), Candida glabrata, Candida tropicalis, and Cryptococcus neoformans, with MICs at which 90% of isolates were inhibited of 0.03, 1, 0.5, and 0.5 microg/ml, respectively.15616275
Salicyl glycoconjugates containing hydrazide and hydrazone moieties The bioassay indicated that the novel compounds had no in vitro fungicidal activity but showed significant in vivo antifungal activity against the tested fungal pathogens. Molecular design and synthesis of novel salicyl glycoconjugates as elicitors against plant diseases. A new series of salicyl glycoconjugates containing hydrazide and hydrazone moieties were designed and synthesized.25259805
Sampangine derivativesPotent inhibitors of Candida albicans biofilm formation and yeast-to-hypha morphological transition by down-regulating biofilm-associated genes Discovery of simplified sampangine derivatives as novel fungal biofilm inhibitors. 29126739
Sargramostim (rh-GM-CSF)Exert beneficial effect in combination with fluconazole in the management of fluconazole-refractory mucosal candidiasis in advanced HIV-positive patients CONCLUSION: In this small pilot study, sargramostim appears to exert a beneficial effect on the mucosal mycoflora and may be a possible alternative as adjunctive therapy in the management of fluconazole-refractory mucosal candidiasis in advanced HIV-positive patients. 11590502
SCH-56592 (SCH) is a novel triazoleVaried activity against itraconazole-susceptible resistant isolate of Aspergillus fumigatus Efficacy of SCH-56592 in a temporarily neutropenic murine model of invasive aspergillosis with an itraconazole-susceptible and an itraconazole-resistant isolate of Aspergillus fumigatus. SCH-56592 (SCH) is a novel triazole antifungal agent with excellent in vitro activity against Aspergillus.9210674
SCY-078Potency against Echinocandin-Resistant Strains of Candida Species Differential Activity of the Oral Glucan Synthase Inhibitor SCY-078 against Wild-Type and Echinocandin-Resistant Strains of Candida Species. SCY-078 (formerly MK-3118) is a novel orally active inhibitor of fungal ?-(1,3)-glucan synthase (GS).28533234
T-2307, a novel arylamidineActivity against Cryptococcus gattii Conclusions: T-2307 shows excellent in vitro and in vivo antifungal activities against C. gattii and would be a promising new candidate for the treatment of cryptococcosis. 28201509
T-2307, novel arylamidinePotent in vitro activity against C. glabrata (geometric mean MIC 0.0135 mg/L),and in vivo efficacy in mice infected with echinocandin-resistant C. glabrata. The novel arylamidine T-2307 demonstrates in vitro and in vivo activity against echinocandin-resistant Candida glabrata.26620102
Terbinafine (SF 86-327)The yeasts showed varying degrees of susceptibility (MICs ranging from 10 to 100 micrograms/ml) except for Candida parapsilosis (MICs 1 to 2 micrograms/ml), strong susceptibility was found for molds (MICs 0.1 to 2 micrograms/ml), especially Scopulariopsis brevicaulis and Sporothrix schenkii (MICs 0.2 microgram/ml), dermatophytes were also highly susceptible to terbinafine (MICs 0.001 to 0.02 microgram/ml). [In vitro spectrum of action of a new antifungal derivative of naftifin: terbinafin (SF 86-327)]. Terbinafine (SF 86-327) is a new antifungal agent derived from naftifine and effective by the oral route.3534767
Tetrazole VT-1161Trichophyton rubrum CYP51 inhibitor with IC50 of 0.14 microM,?growth inhibition with MIC50, MIC90, and geometric mean MIC values of less than or equal to 0.03, 0.06, and 0.033 micro g ml-1, respectively When the activity of VT-1161 was tested against 34 clinical isolates, VT-1161 was a potent inhibitor of T. rubrum growth, with MIC50, MIC90, and geometric mean MIC values of ?0.03, 0.06, and 0.033 ?g ml-1, respectively.28483956
Thiophene-based guanylhydrazones (iminoguanidines)All guanylhydrazones showed significant activity against broad spectrum of clinically important species of Candida spp., Aspergillus fumigatus, Fusarium oxysporum, Microsporum canis and Trichophyton mentagrophytes, which was in some cases comparable or better than activity of voriconazole.: In vivo embryotoxicity on zebrafish (Danio rerio) showed improved toxicity profile of some compounds in comparison to that of voriconazole.Synthesis and evaluation of thiophene-based guanylhydrazones (iminoguanidines) efficient against panel of voriconazole-resistant fungal isolates. However, bis-guanylhydrazone 18 showed better selectivity in terms of therapeutic index values.26867487
Thymol and 2,3-dihydroxybenzaldehyde (2,3-D)Chemosensitizing agents act as synergists to commercial antifungal drugs against tolerant strains of Aspergillus fumigatusChemosensitization prevents tolerance of Aspergillus fumigatus to antimycotic drugs18486603
triazole derivatives containing substituted 1,2,3-triazole-piperdine side chainsThe highly active compounds have MIC values in the range of 0.125 micro g/mL to 0.0125 micro g/mL against Candida albicans and Cryptococcus neoformans Design, synthesis and antifungal activity of novel triazole derivatives containing substituted 1,2,3-triazole-piperdine side chains. They represent promising leads for the development of new generation of triazole antifungal agents.24934573
Triazole-thiazolidinedione hybrids [ (Z)-5-(2,4-dichlorobenzylidene)-3-(2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl)thiazolidine-2,4-dione) (15 c), (Z)-3-(2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl)-5-(furan-3-ylmethylene)thiazolidine-2,4-dione (15 j), and (Z)-3-(2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl)-5-(furan-3-ylmethylene)thiazolidine-2,4-dione (15 r) ]Compounds 15 c, 15 j, 15 r were highly active against Candida albicans, with MIC80 values in the range of 0.03-0.15 microM., compounds 15 j and 15 r were found to be effective against four fluconazole-resistant clinical isolates; From antidiabetic to antifungal: discovery of highly potent triazole-thiazolidinedione hybrids as novel antifungal agents. In an attempt to discover a new generation of triazole antifungal agents, a series of triazole-thiazolidinedione hybrids were designed and synthesized by molecular hybridization of the antifungal agent fluconazole and rosiglitazone (an antidiabetic).25196996
Voriconazole (UK-109496), a new triazole[MIC]90, 0.5 mg/l against Aspergillus fumigatus, MIC90, 1.0 mg/ against Aspergillus nige and 1.0 mg/l against Aspergillus flavus Antifungal activity of a new triazole, voriconazole (UK-109496), against clinical isolates of Aspergillus spp. Voriconazole is a new triazole antifungal agent with potent activity against yeast and molds.11810544
VT-1129MIC ranges between 16-32 micro g/ml against fluconazole dose-dependent, and greater than 64 micro g/ml on resistant isolates of Cryptococcus neoformans, overall MIC was 0.027 micro g/ml, the MIC50 was reported to be 0.05 ?g/ml and 0.25 ?g/ml for dose-dependent (n = 27) and resistant isolates (n = 6), respectively.? Activity of VT-1129 against Cryptococcus neoformans clinical isolates with high fluconazole MICs.27664991
VT-1129 VT-1129 demonstrated potent activities againstCryptococcus neoformans and Cryptococcus gattii with low MIC50and MIC90valuesThe Investigational Fungal Cyp51 Inhibitor VT-1129 Demonstrates Potent In Vitro Activity against Cryptococcus neoformans and Cryptococcus gattii. VT-1129 demonstrated potent activities against bothCryptococcusspecies as demonstrated by low MIC50and MIC90values.26787697
VT-1161 and VT-1129Promising for the treatment of resistant C. glabrata and C. krusei infections VT-1161 and VT-1129 are promising for the treatment of resistant C. glabrata and C. krusei infections.27956419
LMM11, a new oxadiazoleMinimum inhibitory concentration against Candida krusei ranged from 32 to 64 microg/mL with a significant reduction in the colony forming unit (CFU) count (~3 log10), significant reduction in CFU (0.85 log10) in vivoTaken together, these results indicate that LMM11 is a promising candidate for the development of a new antifungal agent for the treatment of infections caused by resistant Candida species such as C. krusei.31935275
Delta-LactonesBroad spectrum of antifungal activity, including against resistant fungal speciesToxicity was dose dependent for the viability of human leukocytes, but none of the compounds was mutagenic, genotoxic, or membrane irritant when evaluated at higher concentrations than MICStructure-based design of Delta-lactones for new antifungal drug development: susceptibility, mechanism of action, and toxicity.30734157
19,20-epoxycytochalasin Q (ECQ) from fungus Xylaria sp. BCC 1067ECQ displayed an antifungal activity with low MIC50 of 410 and 55 mg/l in the model yeast Saccharomyces cerevisiae wild-type and Sc?pdr5 strains, respectively.Combination of ECQ and antifungal azoles displayed promising drug synergy against S. cerevisiae strains expressing multi-drug transporters, thereby providing potential solution for antifungal therapy and chemotherapeutic application.33227681
1,3,4-oxadiazoles bearing 3,4-dihydropyrimidine heterocyclic motifs compoundsFurthermore, results of the antifungal activity tests revealed that compound 4i showed promising activity against all the strains of fungi, Candida albicans, Aspergillus niger, and Aspergillus clavatus, at concentrations of 100, 50, and 100 microgramg/ml, respectively.Compound 4d was found to be the most promising against Escherichia coli (12.5??microgramg/ml), whereas the same compound showed good activity against Staphylococcus aureus at a concentration of 50??microgramg/ml.34169569
1-(2-Hydroxy-3-{[4-(2-propoxyethoxy)benzoyl]oxy}propyl)-4-(4-nitrophenyl)piperazinediium dichloride1-(2-Hydroxy-3-{[4-(2-propoxyethoxy)benzoyl]oxy}propyl)-4-(4-nitrophenyl)piperazinediium dichloride had the highest activity against F. avenaceum (MIC = 14.2 microgramM).All the compounds showed only insignificant toxic effects on human and plant cells.Compounds with a piperazine ring have proved to be promising agents against various pathogens.31518219
T-2307, a novel arylamidineThe ocular T-2307 trough concentration was maintained above the MIC in the infected mice.Given these results in experimental disseminated candidiasis, T-2307 may be an effective treatment against the complication of ocular candidiasis.30753506
echinocandins (anidulafungin, micafungin)In vitro combination of fluconazole with anidulafungin was found to be synergistic (FICI 0.07-0.37) and decreased the MIC range from 4-64 microgramg/mL to 0.5-16 microgramg/mL for fluconazole and from 2-8 microgramg/mL to 0.125-1 microgramg/mL for anidulafungin. Similarly, interactions of fluconazole with micafungin (FICI 0.25-0.5), itraconazole with anidulafungin (FICI 0.15-0.37) and itraconazole with micafungin (FICI 0.09-0.37) were synergistic.The combination of fluconazole and itraconazole with either anidulafungin or micafungin demonstrated synergistic interactions against C. parapsilosis species complex, especially against isolates with elevated MIC values.31715297
RezafunginRezafungin showed excellent in vitro activity against both WT and azole-resistant Candida species, as well as against S. cerevisiae.31539426
4-phenyl-1, 3-thiazol-2-ylMminimum inhibitory concentration against pathogenic fungi was between 0.0625-4 micro g/ml in vitro, could exhibit significant fungicidal activity and inhibit the biofilm formation of C. albicans at 0.5 micro g/ml. In vivo fungal infection model showed that at 10 mg/kg it significantly increased the survival rate of Galleria mellonella.No obvious cytotoxicity to human umbilical vein endothelial cells with the concentration of 4 microgram/mlDevelopment of effective fungicides can not only provide new means for clinical treatment, but also reduce the occurrence of fungal resistance.33117733
Aromatic-rich piperazinesInhibit biofilm formation by C. albicans.Effective treatment of infectious diseases now requires new antimicrobial therapies.33091849
MetyltetraproleActivity against Z. tritici, P. teres, Ramularia collo-cygni, Pyrenophora tritici-repentis, and several other plant pathogenic fungiThe unique behavior of metyltetraprole against the existing QoI-R isolates was confirmed for all tested pathogen species.31769927
Schiff bases of 2-mercaptobenzimidazole were synthesized from 4-(2-(1H-benzo[d]- imidazol-2-ylthio)acetamido)benzohydrazideCompounds 8 (MICpa, an = 2.41, 1.20 microgramM/ml), 10 (MICse, sa = 2.50 microgramM/ml), 20 (MICec = 2.34 microgramM/ml) and 25 (MICca = 1.46 microgramM/ml) showed significant antimicrobial activity against tested bacterial and fungal strainsIn general, the synthesized derivatives exhibited moderate antimicrobial and anticancer activities.30306865
triazole, PC945,PC945 (geometric mean MIC = 0.058 mg/L) was 7.4-fold and 1.5-fold more potent than voriconazole and posaconazole, respectively (both P < 0.01).PC945 was found to be a more potent inhibitor than posaconazole, voriconazole and fluconazole of C. auris isolates collected globally, warranting further laboratory and clinical evaluations.31325309
triazole, PC1244PC1244 exhibited potent inhibition [geometric mean MIC (range), 1.0 mg/L (0.125 to >8 mg/L)] of growth of A. fumigatus strains carrying cyp51A gene mutationsCompound 4d was found to be the most promising against Escherichia coli (12.5 microgram/ml), whereas the same compound showed good activity against Staphylococcus aureus at a concentration of 50 ?g/ml.PC1244 has the potential to become a novel topical treatment of azole-resistant pulmonary aspergillosis.31361006
Gepotidacin, a novel triazaacenaphthyleneGepotidacin was active against all 54 M. genitalium isolates with median and modal MICs of 0.125 mg/L and MIC90 of 0.25 mg/L (range ?0.016-0.5 mg/L).Combination therapy with doxycycline should be clinically studied to assess effect and potential protection against development and/or spread of gepotidacin resistance.32552547
Indole-thiazolidinone conjugates (8a,b; 11a-d) and (14a-k; 15a-h)Compound 15b emerged as a hit in this study with potent broad spectrum antibacterial (MIC: 0.39-0.98 ?g/mL) and antifungal (MIC: 0.49-0.98 ?g/mL) activitiesNovel indole-thiazolidinone conjugates: Design, synthesis and whole-cell phenotypic evaluation as a novel class of antimicrobial agents30317025
Chalcone analogs(chalcone 12)Chalcone 12 showed potent antifungal effects, being able to inhibit the growth of Candida spp. at a concentration of 15.6 micro g mL-1. An in vivo model of VVC showed that chalcone 12 significantly reduces the fungal load.Despite a considerable antifungal activity, the chalcone 12 showed high cytotoxicity in kidney cells lineages Design, synthesis, biological activity and structure-activity relationship studies of chalcone derivatives as potential anti-Candida agents.29674635
FarnesolIn addition, farnesol treatment caused a significant reduction in intracellular iron (152.2 +/- 21.1 versus 116.0 +/- 10.0 mg/kg), manganese (67.9 +/- 5.1 versus 18.6 +/- 1.8 mg/kg), and zinc (787.8 +/- 22.2 versus 245.8 +/- 34.4 mg/kg) (P < 0.05 to 0.001) compared to untreated control cells, whereas the level of cooper was significantly increased (274.6 +/- 15.7 versus 828.8 +/- 106.4 mg/kg) (P < 0.001).This study has demonstrated that farnesol enhances the oxidative stress and reduces the fungal survival strategies.34643421
Compound 3e (4-methoxy-N-butylcinnamamide)Compound 3e (4-methoxy-N-butylcinnamamide) was the most potent (MICrange 0.08-0.16 mg/ml; MFCrange 0.32-0.64 mg/ml) from the set, suggesting a different role of the substituents in ester and amide derivatives.Eleven analogues showed activity against all fungal strains with minimum inhibitory concentrations (MIC) ?1 mg/ml (1a-d, 2e, 3b, 3e, 4, 4a and 5e) and fungicidal concentrations (MFC) ?1 mg/ml (1b, 1d, 3e and 4a), whereas 3 was the less active with both MIC and MFC values above 1 mg/ml.34873847
2- Mercaptomidazoles2-mercaptoimidazoles may be used as potential lead molecules as 14alpha-demethylase inhibitors.Compound 2-(1-(3-hydroxyphenyl)-2- mercapto-1H-imidazol-4-yl)phenol was found to be the most potent compound among all synthesized compounds against tested fungal strains.31020935
Compound 1-i, derived from 3-methylfuran-2-carbaldehydeCompound 1-i, derived from 3-methylfuran-2-carbaldehyde showed the highest antifungal potential with an emphasis on the inhibition of Candida albicans species (MIC = 0.5 micro g/mL) and the highest antioxidant potential.we report the investigation of the antioxidant and antifungal behavior of dimeric naphthoquinones derived from lawsone whose antimicrobial and antioxidant potential has been reported in the literature.31868147
Novel neuchromenin analoguesMoreover, compound 6c also exhibited good activity against C. lunata with EC50 values of 12.7 micro g/mL, and the value was much superior to that of thiabendazole (EC50 = 59.7 micro g/mL).Compounds 6b-c, and 6l showed obvious inhibition activity on each of the fungi at 50 ?g/mL. For the corresponding fungi, 7 of the compounds showed average inhibition rates of >80% at 50 ?g/mL; especially, compounds 6b, 6d-e, and 6i-l displayed more potent antifungal activity against A. solani than that of thiabendazole (a positive control).31009909
Novel miconazole analogues containing seleniumIt is especially encouraging that all the novel target compounds displayed significant antifungal activities against all tested strains. Furthermore, all the target compounds showed excellent inhibitory effects on fluconazole-resistant fungi.Further hemolysis test verified that potential compounds had higher safety than miconazole.In addition, molecular docking study provided the interaction modes between the target compounds and C.alb. CYP51. These results strongly suggested that some target compounds are promising as novel antifungal drugs.32403018
Isatin hybridized 1,2,4-triazole 7aThe active molecule 7a possessed the ability to kill some bacteria and fungi as well as displayed low propensity to induce resistance towards E. coli ATCC25922.Bioactive assay revealed that isatin hybridized 1,2,4-triazole 7a exhibited excellent inhibitory activity against E. coli ATCC 25,922 with an MIC value of 1 ?g/mL, which was 8-fold more potent than reference drug norfloxacin.33839249
Novel 5-phenylthiophene derivativesPreliminary mechanistic studies showed that the potent antifungal activity of compound 17f stemmed from inhibition of C. albicans CYP51.In addition, Compounds 17b and 17f were almost nontoxic to mammalian A549, MCF-7, and THLE-2 cells.Furthermore, the potent compounds 17b and 17f could prevent the formation of fungi biofilms and 17f displayed satisfactory fungicidal activity.34388384
Novel 4-phenyl-4,5-dihydrooxazole derivativesFurthermore, the potent compound 22a could prevent the formation of fungalbiofilms and displayed satisfactory fungicidal activity.Compound 22a was almost nontoxic to mammalian A549, MCF-7, HepG2, and 293T cells.It was especially encouraging that compound 22a displayed significant antifungal activities against eight susceptible strains and seven FLC-resistant strains.34749201
bis-(1,2,3- and 1,2,4)-triazole derivativesMajority of the synthesized compounds exhibited potent antimicrobial activity (MIC 3.9 microg/mL) and promising antifungal activity with the zone of inhibition (ZOI) 1.5-8.2 mm.This substantial growth inhibitory activity of bis-1,2,3- and 1,2,4-triazole derivatives suggested these compounds could assist a new way in the development of lead molecules against microbial infection and antimicrobial resistance investigations.33811989
New Co(II) complexes with thiocarbamoyl-pyrazoline ligandsBoth complexes exhibited fungistatic and fungicidal activity for the yeasts used in the study, demonstrating greater potential for C. glabrata ATCC 2001 and the C. glabrata CG66 isolate with a Minimum Inhibitory Concentration MIC from 3.90 to 7.81 micro g mL-1 and fungicidal action from 7.81 to 15.62 micro g mL-1The complexes inhibited and degraded biofilms by up to 90% and did not present mutagenic and cytotoxic potential at the concentrations evaluated for MIC. Thus, the complexes examined herein suggest promising alternatives for the development of new antifungal drugs.33045593
Kisameet clay (KC)Here, we have extended the known spectrum of activity of KC by demonstrating its efficacy against two major fungal pathogens, Candida albicans and Cryptococcus neoformans33024043
5-fluorouracil, 5-flucytosine5-FC and 5-FU were effective against fifteen fluconazole resistant Candida glabrata strains with an average minimal inhibitory concentration (MIC) of 0.152mg/L and 0.39mg/L, respectively.In this study we reveal the beneficial effect of folinate on antifungal activity of 5-FC as well as the antifungal potential of 5-FU+folinate.31023592
Arylamide derivativesDrug-resistant fungi (C.alb. Strain100, C.alb. Strain103)Most of compounds demonstrate the potent antifungal activity against multiple Candida spp. and A. fum.32220664