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
Designing Functionally Substituted Pyridine-CarbohydrazidesNOverall results suggest that these compounds have the potential to become promising antimicrobial drugs against MDR strains.36615406
Efinaconazole, a novel triazoleFusarium species demonstrated MICs with efinaconazole (0.98 microg/ml)Efinaconazole, a novel triazole, may be a promising candidate for the treatment of superficial Fusarium infections.36447396
Guanylated Hyperbranched Polylysineshyperbranched polylysine (HPL) shows antifungal activities against Candida, especially for drug-sensitive and MDR C. albicans strains, and broad-spectrum antibacterial activities against both Gram-negative and Gram-positive bacteria.The in vitro antifungal activities of HPL3 are further enhanced by the modification of amine groups to form guanylated polylysines (HPL3-Gxs) have potentials as broad-spectrum antimicrobials.35775877
novel isatin-decorated thiazole derivatives(3)-5-Bromo-3-((5-(2-(4-fluoro-3-methylphenyl)hydrazono)-4-methylthiazol-2(5H)-ylidene) hydrazono)indolin-2-one - 7h comopund and 5-Bromo-3-((4-ethoxy-5-(2-(4-fluoro-3-methylphenyl)hydrazono)thiazol-2(5H)-ylidene)hydrazono)indolin-2-one Compound 11f were found to have antifungal activities against Candida albicanshese novel isatin-based compounds were screened for their probable antimicrobial effect on E. coli, MRSA and C. albicans as well as their potential as anti-biofilm formation agents.36046334
NHC 1,3-dibenzyl-4,5-diphenyl-imidazol-2-ylidene silver(I) acetate (SBC3)SBC3 treatment resulted in up to 90% growth inhibition of C. parapsilosis in vitro at the highest test concentration. The determined MIC50 and MIC80 values, representing 15 microg/ml and 25 microg/ml, respectivelyno adverse effect on mammalian protein synthesis.Silver can also contribute to structural damage. Association with cell membranes/walls and formation of pores alters permeability, resulting in ion leakage, and ultimately, cell death. In fungi, demonstrated inhibition of growth via cell cycle arrest and prevention of cell budding in C. albicans in response to silver.35751649
novel 3,4-isoxazolediamide derivativesThe derivative compound B25 was found to have good synergistic effects with fluconazole against azole-resistant candidiasisto avoid potential mammalian toxicity.promising lead compound for drug discovery targeting fungal Hsp90 and deserves further investigation.36029272
Non-Antibiotic Antimony-Based AntimicrobialsAntifungal effect of new tetraphenyl-antimony(V) cyanoximates determined using a disc-diffusion assay against selected two human fungal pathogensAntifungal studies showed that SbPh4(MCO) was the only compound to inhibit the growth of both fungal pathogens C. neoformans and C. albicans, also known for their increasing resistance to antimicrobials. The other compounds inhibited the growth of C. neoformans but not C. albicans.36363997
new 2-substituted-4-amino-quinolines and -quinazolineThe mechanism studies showed that compound III11 (N,2-di-p-tolylquinolin-4-amine hydrochloride) exhibited potent and broad-spectrum antifungal activities with MIC values of 4-32 microg/mL.These results suggest that some 4-aminoquinolines may serve as new and promising candidates for further antifungal drug discovery.35788035
novel compounds containing 1,2,3-triazole side(2R,3S)-3-[1-(4-chloro-2-fluorophenyl)-1H-1,2,3-triazol-4-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)butan-2-ol compound 9A16 displayed excellent antifungal and anti-drug-resistant fungal ability (MIC80 = 0.0156-8 microg/mL). compound 9A16 showed powerful in vivo efficacy on mice systematically infected with Candida albicans SC5314, Cryptococcus neoformans H99, fluconazole-resistant C. albicans 100, and Aspergillus fumigatus acceptable safety profileWith favorable pharmacokinetics, an acceptable safety profile, and high potency in vitro and in vivo, compound 9A16 is currently under preclinical investigation.36512715
4,4'-dihydroxyazobenzene, a compound and azobenzene derivativeshese compounds prevented the growth of both fluconazole-susceptible and fluconazole-resistant Candida albicans and Candida auris strains.36403201
novel indole and indoline derivativesThe results showed that title compounds exhibited good antifungal effect on Azole-resistant C. albicansinhibit the biofilm formation and hyphae growth of C. albicans through the Ras-cAMP-PKA signaling pathway.35661686
The anhydride of ferrocenyl-substituted pyrazole, namely, (S)-(3-(3-(carboxyamino)-3H-pyrazol-4-yl)cyclopenta-1,3-dien-1-yl)(cyclopenta-1,3-dien-1-yl)ironThe synthesized compound was found to be biological active in the range of 85-95 microg/ml against various human pathogenic Gram-positive, Gram-negative, and fungal microbial strains.The study demonstrations that synthesized ferrocenyl-substituted pyrazole in today's situation is the encouraging antimicrobial mediator against the human pathogens.35949692
trimethoxybenzoic acid derivatives3,4,5-Trimethoxy-N-(2-(4-methylpiperazin-1-yl)ethyl)benzamide derivative- Susceptibility tests were performed by the broth microdilution method based on the Clinical and Laboratory Standards Institute (CLSI); M27A-3 for yeasts (C. albicans) and M38-A2 [42] for filamentous fungi (A. fumigatus and T. rubrum)these results show the potential of simple trimethoxybenzoic acid derivatives as a source of feasible efflux pump (EP) inhibitors.36430942
6-hydroxy-1,2,3,4-tetrahydroquinolineCommercially available 6-hydroxy-1,2,3,4-tetrahydroquinoline (compound 1) was treated with 1-bromoalkanes or 1-iodoalkanes in the presence of K2CO3 to yield compounds. This compound derivative display potent and broad-spectrum antimicrobial activity against Gram-positive and Gram-negative bacteria, as well as fungiIn conclusion, successfully designed and synthesized a series of amphiphilic tetrahydroquinoline derivatives as effective broad-spectrum antimicrobial agents.36088756
EGFR inhibitor osimertinib mesylate (OSI)(OSI) potentiates azole efficacy against diverse fungal pathogens and overcomes azole resistance. Mechanistic investigation revealed a conserved activity of OSI by promoting intracellular fluconazole accumulation via inhibiting Pdr5 and disrupting V-ATPase function via targeting Vma1 at serine 274, eventually leading to inactivation of the global regulator TOR.the identification of OSI as a dual action antifungal with co-targeting activity proposes a potentially effective therapeutic strategy to treat life-threatening fungal infection and overcome antifungal resistance.35452875
quinolinequinones (QQs) derivative7-chloro-6-[4-(3-methylphenyl)piperazin-1-yl]-5,8-dihydroquinoline-5,8-dione QQ3 and QQ4 7-chloro-6-[4-(4-methylphenyl)piperazin-1-yl]-5,8-dihydroquinoline-5,8-dione show two times more activity against fungal strains Candida albicans and Candida parapsilosis. all QQs except QQ5 displayed excellent antifungal activity against the fungi Candida albicansIn this study, we investigated the bactericidal effects of QQ3 against methicillin-resistant Staphylococcus aureus (MRSA) and Candida albicans strains. The findings of this study suggest that a significant bactericidal effect was seen with all tested 1 35921788
1,4-quinone molecules fused with heteroatom derivativestwo quinolinequinones derivative (QQ7 and QQ8 4.88MIC) displayed better antifungal activity against C. albicans and C. parapsilosis.the activity of these compounds against three different strains of Candida fungi (C. albicans, C. parapsilosis, and C. tropicalis) and Gram-positive and Gram-negative pathogenic bacteria were investigated, searching for potential lead compounds.36290056
C. neoformans 5-aminoimidazole-4-carboxamide ribonucleotide (AICAR) transformylase/5'-inosine monophosphate cyclohydrolase (ATIC), a bifunctional enzymea bifunctional enzyme that catalyzes the final two enzymatic steps in the formation of the first purine base inosine monophosphate.. Overall, our results validate ATIC as a promising antifungal drug target.36063996
Compounds based on cobalt bis-dicarbollide [COSAN]The presented data prove that metallacarborane derivatives are effective against clinical isolates of Candida albicans, even those resistant to systemic drugs, and show synergistic potential in combination with amphotericin Blow toxicity against human cells and Danio rerio embryos.the investigations of the broad spectrum and valuable future medical applications of metallacarboranes, especially in the fight against drug-resistant pathogens.36217958
baicaleinThese results indicated that baicalein could increase intracellular oxidative damage by upregulating the expression of Cpd2p so as to inhibit the growth of C. albicans,urther in-depth studies revealed that CPD2 disruption reduced the activation of C. albicans metacaspase and partially restored the mitochondrial membrane potential reduction caused by the treatment of baicalein, which indicated that CPD2 was involved in the apoptosis induced by baicalein. Which provides new insights for investigating the antifungal target of baicalein.36055797
Combined applications of Spent mushroom substrate (SMS) and dicyandiamide compoundCompared to the control treatment, the combined applications of SMS and dicyandiamide significantly decreased soil carbendazim content by 38.14%he SMS applications into fungicide-contaminated soils could generate double-edged sword effects of facilitating fungicide dissipation. dicyandiamide with SMS might be an effective strategy to decrease the negative effect of health risk.36596378
two terpyridine ligands 4'-(4-N,N'-dimethylaminophenyl)-2,2':6',2?-terpyridine (L1) and 4'-(4-tolyl)-2,2':6',2?-terpyridine (L2)Both compounds L1 and L2 exhibited remarkable inhibitory activities against bacteria, Escherichia coli and Staphylococcus aureus at MIC values 6.25 and 3.125 microg/ml, respectively. in silico molecular docking studies were ascertained with bacterial DNA gyrase and fungal demethylase.he toxicity of L1 and L2 was checked using Drosophila melanogaster. The toxicity analysis suggest both the dyes are non-cytotoxic in nature.The binding constant calculations at different temperature confirmed that the ligand has antimicrobial and antifungal activities36562209
Lipid-Modified Chitin-Binding DomainsLysM-AmBisome exhibited a dramatic enhancement of antifungal activity toward Trichoderma viride and Cryptococcus neoformans, demonstrating the marked impact of displaying a cell-wall binder protein on the targeting ability of antifungal liposomal formulations.(LysM-Pal) exhibited negligible cytotoxicity to mammalian cells and can be easily anchored to yield LysM-presenting AmBisome (LysM-AmBisome).simple strategy with enzymatic protein lipidation provides a potent approach to upgrade other types of lipid-based drug formulations.36066555
Novel 3-(2-(3-(Substituted benzyloxy)oxetan-3-yl)-3-fluorophenoxy)-8-fluoro-2-methylquinoline Derivativescompound 3-(2-(3-(benzyloxy)oxetan-3-yl)-3-fluorophenoxy)-8-fluoro-2-methylquinoline (9a) showed good activity against P. mirabilis, B. subtilis, and A. niger with MIC 31.25 microM; compound 3-(2-(3-((4-bromobenzyl)oxy)oxetan-3-yl)-3-fluorophenoxy)-8-fluoro-2-methylquinoline 9b showed good activity for P. mirabilis, S. albus, and A. niger with MIC 62.5 microM; 4-chlorobenzyloxy in compound 3-(2-(3-((4-chlorobenzyl)oxy)oxetan-3-yl)-3-fluorophenoxy)-8-fluoro-2-methylquinoline (9c) which showed good activity against P. mirabilis with MIC 62.5 microM and moderate activity against A. niger; compound 8-fluoro-3-(3-fluoro-2-(3-((4-methylbenzyl)oxy)oxetan-3-yl)phenoxy)-2-methylquinoline (9d) which showed good activity against P. mirabilis and A. niger with MIC 62.5 microM. Against A. niger compound 3-cyanobenzyloxy in 8-fluoro-3-(3-fluoro-2-(3-((3-cyanobenzyl)oxy)oxetan-3-yl)phenoxy)-2-methylquinoline (9f) showed good activity with MIC 62.5 microM; compound 3-(2-(3-((3,5-difluorobenzyl)oxy)oxetan-3-yl)-3-fluorophenoxy)-8-fluoro-2-methylquinoline (9h), which showed good activity against P. mirabilis and A. niger with MIC 31.25 and 62.5 microM, respectively. 6-fluoropyridin-3-yl-methoxy in 8-fluoro-3-(3-fluoro-2-(3-((6-fluoropyridin-3-yl)methoxy)oxetan-3-yl)phenoxy)-2-methylquinoline (9i), which showed good activity against A. niger with MIC 62.5 microM.Cytotoxicity tests of 3-(2-(3-(substituted benzyloxy)oxetan-3-yl)-3-fluorophenoxy)-8-fluoro-2-methylquinoline (9aThe newly synthesized oxetanyl-quinoline derivatives were evaluated for in vitro antibacterial activity against Escherichia coli (NCIM 2574), Proteus mirabilis (NCIM 2388), Bacillus subtilis (NCIM 2063), Staphylococcus albus (NCIM 2178), and in vitro antifungal activity against Aspergillus niger (ATCC 504) and Candida albicans (NCIM 3100) show good inhibition and can use as novel compound against antimicrobial resistance36570236
chelerythrine combined with fluconazoleA broth microdilution assay was used to reveal the antifungal activity of chelerythrine combined with fluconazole against C. albicans and the preformed biofilm. A fractional inhibitory concentration index model was used to evaluate the interaction. Chelerythrine strongly synergized with fluconazole against fluconazole-resistant C. albicans and the biofilm preformed for less than 12 h.Chelerythrine could reverse the drug resistance of resistant C. albicans and its biofilm to fluconazole, providing new insights for overcoming the drug resistance of C. albicans.36111728
new chiral triazole fungicide mefentrifluconazoleThe results suggest that triazole resistance in A. fumigatus could be resulted from the selection of mefentrifluconazole at concentrations larger than 2 mg L-1Mefentrifluconazole should be applied within the dosage recommended by good agricultural practice to avoid the resistance in A. fumigatus in soil. This also may be applicable to other triazole fungicides.36205310
ipflufenoquin, with a new antifungal olorofimEffective against- Azole resistance in Aspergillus fumigatusThe use of the recently authorized fungicide ipflufenoquin, which shares its mode-of-action with a new antifungal olorofim, underscores the need for risk assessment for dual use of antifungals.36283187
Compounds 1c (alpha-asarone-related) and 5b (with a pyrrolic core) [Fibrate-Based Compounds and Substituted Pyrroles ]Inhibit the Enzyme 3-Hydroxy-methyl-glutaryl-CoA Reductase of Candida glabrata (CgHMGR), Thus Decreasing Yeast Viability and Ergosterol SynthesisFuture studies are needed to modify the structure of the two present test compounds to obtain safer and less toxic antifungals. Moreover, it is important to carry out a more in-depth mechanistic approach.According to the docking analysis, the inhibitory effect of 1c and 5b could possibly be mediated by their interaction with the amino acid residues of the catalytic site of the enzyme. Since 1c displayed higher binding energy than alpha-asarone and 5b, it is the best candidate for further research, which should include structural modifications to increase its specificity and potency.35377226
amphotericin B (AmB)-loaded nanoemulsion (NE) (NEA) [sunflower oil and cholesterol as the oily phase, polyoxyethylene 20 cetyl ether (Brijcontrol of C. auris infections and resistance as well as decrease the side effects of this drugNEA had a better antifungal profile against systemic infection in G. mellonella. It is concluded that the alternative model proved to be an efficient in vivo assay to determine the toxicity and evaluate the therapeutic property of free AmB and NEA in systemic infections caused by C. auris.34662607
combination effect of AZD8055 and fluconazoleSynergism between AZD8055 and fluconazole was observed in six strains (60%) of Candida spp., resulting in reversion of fluconazole resistance. Synergistic combinations resulted in 4-fold to 256-fold reduction of effective MICs of AZD8055 and azoles.In summary, the results suggested that AZD8055 combined with azoles may help to enhance the antifungal susceptibilities of azoles against pathogenic fungi and had the potential to overcome azole resistance issues.35019705
derivative A1Cl of 2-chloro-N-phenylacetamideA1Cl inhibited in vitro biofilm formation at all concentrations tested (1/4MIC to 8 Conclusions: The results suggest that A1Cl is a promising antifungal agent. Furthermore, this activity is related to attenuation of expression of virulence factors and antibiofilm effects against C. tropicalis and C. parapsilosis.35179275
Boric acidboric acid inhibited C. albicans hyphal formation and reduced mature biofilm biomass and metabolic activity in all isolates in a dose-dependent mannerOverall, our findings illustrate that boric acid is broadly effective at inhibiting growth across many isolates and morphologies, which could explain why it is an effective treatment for RVVC.35446135
NitroxolineMIC50/90 of nitroxoline was 2/2 mg/L (MIC range 0.25-4 mg/L)In conclusion, isolates of different Candida species are highly susceptible to nitroxoline, which could be a promising antimicrobial to treat candiduria caused by multidrug resistant yeasts.35543103
15 N [Cobalt Ferrite (0.3 CoFe2O4) + Silver chromite (0.7 Ag0.5Cr2.5O4)]against M. luteus. Concerning antifungal activity, C. albicans was the most susceptible fungal speciesThe tested compounds could be attractive and alternative antibacterial compounds that open a new path in chemotherapy.35624524
juglone (5-hydroxy-1,4-naphthoquinone)against both fluconazole-resistant and susceptible Candida isolatesJuglone increased the antifungal activity of fluconazole; however, no synergism effects were observed for any combination, and only an insignificant effect was found against all tested Candida species.35701335
chlorhexidine acetate in combination with fluconazoleagainst suspensions and biofilms of Candida aurisConclusion: The combination therapy of fluconazole and chlorhexidine acetate provides a new potential strategy for the treatment of clinical Candida auris infection.34674944
Heat shock protein 90 (Hsp90)/Histone deacetylase (HDAC)dual inhibitors for the treatment of azoles-resistant Candida albicansTherefore, Hsp90/HDAC dual inhibitors represent a new strategy for the development of novel antifungal therapeutics to combat azole-resistant candidiasis.34742014
Recombinant MyeloperoxidaseTaken together, the data suggest that rMPO purified from a stably expressing human cell line is a new class of antimicrobial agents with the ability to kill a broad spectrum of pathogens, including bacteria and fungi with or without drug resistance.35019674
Compounds 5b (Z)-3-(3-hydroxyphenyl)-5-((1-methyl-1H-indol-3-yl)methylene)-2-thioxothiazolidin-4-one and 5g (Z)-3-[5-(1H-Indol-3-ylmethylene)-4-oxo-2-thioxo-thiazolidin-3-yl]-benzoic acid as well as 5h (Z)-3-(5-((5-methoxy-1H-indol-3-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)benzoic acidAll compounds demonstrated a higher degree of antifungal activity than the reference drugs bifonazole (6-17-fold) and ketoconazole (13-52-fold).Conclusion: Compounds 5b (Z)-3-(3-hydroxyphenyl)-5-((1-methyl-1H-indol-3-yl)methylene)-2-thioxothiazolidin-4-one and 5g (Z)-3-[5-(1H-Indol-3-ylmethylene)-4-oxo-2-thioxo-thiazolidin-3-yl]-benzoic acid as well as 5h (Z)-3-(5-((5-methoxy-1H-indol-3-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)benzoic acid can be considered as lead compounds for further development of more potent and safe antibacterial and antifungal agents.35164333
polypyridyl iridium(III) complexespotent agents against resistant Candida albicansThis study may pave the way for the development of novel antifungal agent based upon polypyridyl iridium(III) complex to combat antifungal resistance.35276422
Pseudolaric Acid A Combined with Fluconazoleagainst Candida albicans via Inhibition of Adhesion and Yeast-To-Hypha TransitionIn conclusion, these findings demonstrate, for the first time, that the combination of PAA and FLC has an improved antibiofilm effect against the formation of C. albicans biofilms by inhibiting adhesion and yeast-to-hypha transition; this may provide a novel therapeutic strategy for treating C. albicans biofilm-associated infection.35297651
pyrvinium pamoate (PP)PP inhibited C. auris replication in macrophages, which is a relevant host niche for this yeast pathogen.Our study offers a new avenue for therapeutic development against drug-resistant C. auris, shows how complex metabolic dysfunction can be caused by a single compound triggering antifungal inhibition, and provides insights into the metabolic needs of C. auris in immune cell environments.35412372
chlorogenic acidagainst strains of Candida spp. resistant to fluconazoleWe concluded that chlorogenic acid has potential use as an adjuvant in antifungal therapies, due to its anti-Candida activity and ability to interact with important drug targets.35575783
Chrysosporium sp. HSXSD-11-1, Cladosporium sp. HSXSD-12 and Acrostalagmus luteoalbus CH-6the crude extracts of CH-6 displayed the strongest antimicrobial activities with 72.3-84.8% growth inhibition against C. albicans and Aeromonas salmonicida.This study further demonstrates the great potential of Antarctic fungi in the development of new compounds and antibiotics.35621985
calcium supplementation combined with iron deficiencycauses dramatic growth inhibition of the human fungal pathogens Aspergillus fumigatus, Candida albicans, and Cryptococcus neoformansThus, there is a mutual effect between iron and calcium in fungal pathogens, and the combination of calcium with an iron chelator could serve to improve antifungal therapy.35674440
Cold atmospheric plasma (CAP)CAP irradiation significantly inhibited the fungal growth by 25.83 to 89.10%, reduced fungal cell viability by 11.68 to 87.71%, disrupted cellular membranous organelles and structures of the fungal hyphae, and suppressed efficiently the expression of HSP90 gene by 2 folds in 210 s exposure.Taken together, our results demonstrated that CAP is an efficient tool with potential in-vivo therapeutic applications against chronic dermatophytosis caused by T. rubrum due to its effectiveness, harmless, and ease of access.35676321
Thiadiazole-Based MoleculesPromising Inhibitors of Black Fungi and Pathogenic BacteriaFurthermore, a molecular docking study was achieved on the synthesized compounds, of which compounds 2, 6, and 7 showed the best interactions with the selected protein targets.35684551
4-phenyl-4,5-dihydrooxazole derivativesantifungal activities against eight susceptible strains and seven FLC-resistant strains. Furthermore, the potent compound 22a could prevent the formation of fungalbiofilms and displayed satisfactory fungicidal activity.Moreover, pharmacokinetic studies in SD rats showed that compound 22a exhibited pharmacokinetic properties with a bioavailability of 15.22% and a half-life of 4.44 h, indicating that compound 22a is worthy of further study34749201
3-thiophene derivativesshowed excellent inhibitory activity against pathogenic and drug-resistant fungi. In addition, the preferred compound 21b could prevent the formation of fungal biofilms and displayed satisfactory fungicidal activity.These results strongly suggested that compound 21b is worthy of further study as a potential azole inhibitor.35255313
4,5-Diarylisoxazole DerivativesCombination Treatment of Azole-Resistant CandidiasisThese data support the feasibility of targeting fungal Hsp90 as a promising antifungal strategy and further development of compound A17 as a valuable research probe for the investigation of fungal Hsp90.35298171
compound 2a11compound 2a11 can inhibit the growth of azole-resistant strains 103 with the MIC80 of 1 microg/mL.Collectively, this work identifies a new covalent allosteric site of CaFBA and discovers the first generation of covalent inhibitors for fungal FBA with potent inhibitory activity against resistant fungi, establishing a structural foundation and providing a promising strategy for the design of potent antifungal drugs.35099959
berberine hydrochlorideagainst fluconazole-resistant Candida albicansConclusion. BH affects multiple target genes in diminishing the resistance of C. albicans strains to fluconazole. This effect may be related to the action of BH on the HOG-MAPK pathway.35679157
Benzylic Dehydroxylation of Echinocandin Antifungal DrugsRestores Efficacy against Resistance Conferred by Mutated Glucan SynthaseThis study describes the first example of a chemical modification strategy to restore the efficacy of echinocandin drugs, which have a critical place in the arsenal of antifungal drugs, against resistant fungal pathogens.35347986
Minocycline (MIN) and azolesin vitro combination of MIN with ITR, VOR or POS showed satisfactory synergistic effects against 8 (80%), 1 (10%), and 9 (90%) strains, respectively. Moreover, combined use of MIN with azoles decreased the minimum inhibitory concentration (MIC) range from 5.33-16 microg/ml to 1-16 microg/ml for ITR, from 0.42-16 microg/ml to 0.21-16 microg/ml for VOR, and from 1.33-16 microg/ml to 0.33-16 microg/ml for POS.Conclusions: The present study demonstrated that combinations between MIN and azoles lead to synergistic antimicrobial effects on Scedosporium and Lomentospora species, while showing a potential for overcoming and preventing azole resistance.35016611
olorofimInhibition of azole-resistant Aspergillus fumigatus biofilm at various formation stagesConclusions: This is the first known study to demonstrate the antibiofilm activity of olorofim, voriconazole and amphotericin B against azole-resistant A. fumigatus.35289361
Jerveratrum-Type Steroidal AlkaloidsJervine exhibited broad-spectrum antifungal activity and was effective against human-pathogenic fungi, including Candida parapsilosis and Candida krusei. It was also effective against phytopathogenic fungi, including Botrytis cinerea and Puccinia recondita. Jervine exerted a synergistic effect with fluconazole.Therefore, jervine, a jerveratrum-type steroidal alkaloid used in pharmaceutical products, represents a new class of antifungals active against mycoses and plant-pathogenic fungi.35019680
Helja with fluconazole (FLC)The Helja + FLC combination exhibited an inhibitory effect of fungal growth about three times greater than the sum of both compounds separately and inhibited fungal morphological plasticity, an important virulence attribute associated with drug resistance. Cells treated with Helja + FLC showed morphological changes, nucleus disintegration and formation of multimera structures, leading to cell collapse.Conclusions: Our findings indicate that the Helja + FLC combination exhibited a potent antifungal activity based on their simultaneous action on different microbial cell targets.35332971
Delphinium cashmerianum L. (Daidzein compound)Upon analysis, we obtained 5 compounds that were efficiently binding to the drug targets. However, after performing exhaustive molecular docking and molecular dynamic simulation (MDS) analysis, it was observed that Daidzein compound is bound to drug targets more efficiently.Conclusion: The results showed that these plant extracts exhibit antimicrobial activity and ethyl acetate extract proved to exhibit the most effective antibacterial and antifungal properties.35167935
compounds 14a-2 and 20b-2Among of them, target compounds 14a-2 and 20b-2 not only possessed the excellent broad-spectrum anti-fungal activity (MIC50, 0.125-2 Microg/mL), but also maintained the anti-drug-resistant fungal activity (MIC50, 1-4 Microg/mL)In addition, we also discovered that compounds 14a-2 and 20b-2 with low toxic and side effects could exert the excellent therapeutic effect in mice model of fungal infection, which was worthy for further in-depth study.34772530
thiosemicarbazone derivative 19ak as a metal chelator19ak exhibits minimal cytotoxicity and potent activity against either azole-sensitive or azole-resistant fungal pathogens, inhibits fungal ribosome biogenesis mainly by disrupting intracellular zinc homeostasisThis study provides the basis of thiosemicarbazone derivative 19ak as a metal chelator for the treatment of fungal infections.35412374
BDDE-Inspired Chalcone Derivativeschalcones 13 and 14 showed promising antifungal activity against the dermatophyte clinical strain of Trichophyton rubrumBDDE-Inspired Chalcone Derivatives to Fight Bacterial and Fungal Infections35621966
sertraline with fluconazoleluconazole with sertraline (FICI =0.5), where a synergistic effect was observed against all resistant C. glabrata and ATCC strains with a >2-log10 CFU/mL reduction caused by combination compared with a single active agent of fluconazole after 24 hours of incubationConclusion: Our data suggest that blocking active efflux pumps by sertraline may be considered the probable mechanism of synergism with fluconazole. The combination of sertraline with fluconazole could be a promising remedy for treatment of infections caused by resistant C. glabrata.35181564
eucalyptol in combination with antifungalsThe geometric mean MBIC of amphotericin B, itraconazole, nystatin and eucalyptol were 3.93 Microg/mL, 12.55 Microg/mL, 0.75 Microg/mL and 798 Microg/mL, respectively. Eucalyptol interacted synergistically with amphotericin B, itraconazole and nystatin against 12.5, 10, and 22.5% of isolates, respectively.Eucalyptol demonstrated promising activity against biofilm of C. albicans when tested alone or combined with antifungal drugs.35508567
benzbromaronepotential folate inhibitors of Candida albicansBased upon the molecular docking simulation-based virtual screening followed by the molecular dynamic simulation of the macromolecular complex, benzbromarone has been identified as a potential anti-folate agent for the development of a novel therapy for the treatment of candidiasis.35716240
surfactinexerted antifungal effect against Candida albicansOur data demonstrate that surfactin significantly influences the physiology and gene transcription of C. albicans, and could contribute to the development of a novel innovative complementary therapy.35671583
octenidineagainst emerging echinocandin-, azole- and multidrug-resistant Candida albicans and Candida glabrataConclusion: These results encourage consideration of the well-tolerated antiseptic molecule OCT in the eradication of emerging (multidrug) resistant C. albicans and C. glabrata.35134551
Ent-hardwickiic acid from C. pubiflora and its microbial metabolitesAll the diterpenes showed fungistatic effects (ranging from 19Ent-hardwickiic acid from C. pubiflora and its microbial metabolites are more potent than fluconazole in vitro against Candida glabrata34995375
adamantane derivativesfive derivatives (6, 7, 9, 14a, and 14b) displayed the potent activities against the different isolates tested (MIC <8 Microg/ml with fungi) compared with Ciprofloxacin (CIP) and Fluconazole (FCA), showed fungicidal effects based on (MBCs and MFCs) and the time-kill assay. The most active adamantane derivatives 7 and 14b exhibited a synergistic effect of SFIC = 0.5 with CIP and FCA against the bacterial and fungal isolates.Finally, the in-silico analysis predicted that the most active derivatives had good drug-likeness and safe properties.35716118
Dicliptera roxburghianaFor antifungal assay, DRME and DRHF were potently active and showed more than 70% fungal growth inhibition where as DRCF and DRBF were also displaying appreciable inhibition.Cytotoxic measurements were very good for DRME, DRHF and DRAF with LD50 values 215, 199 and 392 Microg/ml respectively.These results confirmed antimicrobial and cytotoxic potential of the plant and all its derived fractions. Hence it can be concluded that plant contain some important compounds that can be used as antimicrobial source for the treatment of different infectious disease.35221269
spirooxindole-pyrrolidine heterocyclic hybridsDPA-3, has potent antifungal activity without inducing mammalian cell cytotoxicity. Furthermore, DPA-3 significantly reduced hyphal and biofilm formation of Candida albicans ATCC 10231 strain, out-competing two FDA approved antifungal drugs.The results of our study conclude that DPA-3 is a compelling candidate for further development as an antifungal drug.35512603
gallic acid (GA)GA presented minimum inhibitory concentrations ranging from 16 to 72 Microg/ml, causing alterations of the membrane integrity and mitochondrial transmembrane potential, production of reactive oxygen species and externalization of phosphatidylserineConclusion: GA has potential antifungal activity against Candida spp.35354285
indole and indoline derivativesagainst Candida albicans as potent antifungal agentsThe results showed that title compounds exhibited good antifungal effect on Azole-resistant C. albicans. Further mechanism study demonstrated that S18 could inhibit the biofilm formation and hyphae growth of C. albicans through the Ras-cAMP-PKA signaling pathway.35661686
Pyridothienopyrimidine DerivativesCompounds 3a, 5a and 9b displayed broad spectrum antimicrobial activity with MIC ranges of 4-16 Microg/mL and potent cytotoxic activity with IC50 ranges of 1.17-2.79 MicroM. In addition, they provided suppressing activity against EGFR with IC50 ranges of 7.27-17.29 nM, higher than that of erlotinib, IC50 = 27.01 nM.All new compounds were evaluated against five bacterial and five fungal strains.35164067
2,5-Disubstituted Pyridineas an Inhibitor of Candida albicans Erg11This work characterizes the antifungal activity of a 2,5-disubstituted pyridine against C. albicans, supporting the mining of existing chemical collections to identify compounds with novel antifungal activity.35531664
analogues of Panax stipulcanatus saponinIn vitro antifungal activity results indicated that analogue 2 combined with fluconazole showed synergistic antifungal activity against fluconazole-resistant Candida albicans, with MIC50 values 31.80 Microg/mL and FICI values 0.32. intermediate compounds 16 and 17 revealed synergistic antifungal activity against susceptible Candida albicans when combined with fluconazole, with MIC50 values 1.43 Microg/mL and 1.59 Microg/mL, FICI values 0.29 and 0.32, respectively.synergistic antifungal activity of analogues of Panax stipulcanatus saponin against fluconazole-resistant Candida albicans35552063
Arylamidine T-2307the MIC of T-2307 was found to be 0.005 microg mL-1 against C. tropicalis DSM 11951 and C. tropicalis.T-2307 did not affect cell viability on PNT1A cell linethese results provide new information on T-2307, indicating this compound as a new and promising alternative therapeutic option for the treatment of Candida infections.36555687
beta-Nitrostyrene derivativesThe results show that beta-Nitrostyrene derivatives inhibited the growth of different species of human pathogenic Candida, particularly the highly prevalent C. albicans, C. glabrata and the emerging pathogenic C. auris species.beta-Nitrostyrene derivatives impact cell wall morphology, enhance ROS generation and modulate drug efflux. Collectively this study reveals that beta-Nitrostyrene derivatives have strong antifungal potential with a particular mode of activity similar to known cell wall perturbing antifungal agents35932582
Hydroxyethyl NaphthalimidesThese prepared naphthalimides showed better antifungal potency than fluconazole towards some tested fungi including Aspergillus fumigatus, Candida tropicalis and Candida parapsilosis 22019. Especially, thioether benzimidazole derivative with excellent anti-Candida tropicalis efficacy (MIC = 4 microg/mL)possessed low cytotoxicity, safe hemolysis level and less susceptibility to induce resistance.antifungal potency promoted the production and accumulation of reactive oxygen species (ROS) in cells, which destroyed the antioxidant defence system, led to oxidative stress with lipid peroxidation, loss of glutathione, membrane dysfunction and metabolic inactivation, and eventually caused cell death. The chemical and dynamic antifungal synergistic effect initiated by hydroxyethyl naphthalimides was a reasonable treatment window for prospective development.36500547
adamantane derivativesMIC of <8 microg/ml with fungi) compared with Ciprofloxacin (CIP) and Fluconazole (FCA).interaction of DNA gyrase and topoisomerase IV enzymes with the compound Derivative exhibited potent antimicrobial activity using in vitro biochemical assays and gel-based DNA-supercoiling inhibition method35716118
hexyl-aminolevulinate ethosomes (HAL-ES)No survival was observed after 6 h of incubation with 20 mM HAL, and growth inhibition was noted at 2.5 to 10 mM HAL against Candida albicans. The results showed that HAL-mediated aPDT killed approximately 66.7% of C. albicans cellsHAL-ES inhibits protein translation by disrupting zinc homeostasis in C. albicans. Hence, provides a novel and effective therapeutic strategy against C. albicans biofilm but also proposes a new strategy to resolve C. albicans biofilm infection by disrupting zinc homeostasis.36301105
volatilomes nest microbiome of the Namibian, social spider Stegodyphus dumicolaThe growth of P. lilacinum was inhibited by the volatilome of Streptomyces sp. and Aureobasidium sp.The antimicrobial activities of five spider nest microbiome member volatilomes (Massilia sp. IC2-278, Massilia sp. IC2-477, Sphingomonas sp. IC-11, Aureobasidium sp. CE_32, and Streptomyces sp. IC-207) against two putative spider pathogens (B. thuringiensis and P. lilacinum) were tested to prove a potential role in pathogen defense36073497