| ENTITY |
POTENCY |
SAFETY_INFORMATION |
EVIDENCE |
PMID |
| 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 agent | Potential 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-oxazoles | Activity 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-ols | Broad-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) analogues | Antibacterial 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 2 | Inhibited 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/mL | | Synthesis 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 Derivatives | Overall 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-1 | | Synthesis 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'-methoxychalcone | Activity against fluconazole-resistant Candida albicans | | To 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 derivatives | The 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 derivatives | The 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 derivatives | Antibacterial 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 maleimides | Of 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 hydrochlorides | All 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 A | Completely 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 derivatives | MIC values ranging from 15.6 to 0.975 microg/mL | | Synthesis and investigation of novel benzimidazole derivatives as antifungal agents. | 27301676 |
| Ambroxol Hydrochloride Combined with Fluconazole | Ambroxol 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 inhibitors | Combinations 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 Fidelity | 26573415 |
| Anthracene-9-carboxylic and niflumic acid | Effect 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 Derivative | Activity 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 compounds | Broad-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 microM | The 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 |
| ASP2397 | ASP2397 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 |
| Azoxybacilin | Broad 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 models | A screening assay based on host-pathogen interaction models identifies a set of novel antifungal benzimidazole derivatives. | 21746957 |
| Benzofuran derivatives | Antifungal 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-bishydrazones | Antibacterial 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 fungi | Minimal 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 |
| Bromoquinol | Active against Aspergillus fumigatus | | The 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 carbohydrate | Inhibited 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 fluconazole | Showed 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-685,818 | Activity against Cryptococcus neoformans | | Synergistic 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 neoformans | 10681348 |
| 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.H2O | | Antifungal 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 triazole | CS-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/haemofungin | Inhibits the growth of pathogenic Aspergillus, Candida, Fusarium and Rhizopus isolates at micromolar concentrations | Only 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-arylthiazoles | Five 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 triazole | MICs 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 |
| D75-4590 | Potent 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)indoles | Antitumour and antifungal activity | Antifungal 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 2 | Compound 1 showed higher activity (% = 100 at 4 ?g/ml) than Compound 2 (MIC90 = 16 ?g/ml) against Candida spp | | Sulfone 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 eugenol | Antifungal 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 |
| F901318 | A. 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 inhibitor | Efficacy 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 agent | antagonist 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 |
| Glabridin | Significant 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 polymethacrylates | The most potent compound kills 99.98% of S. aureus and 82.2% of C. albicans at a concentration of 128 mg/L | | Searching 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) analogues | Four 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 peroxide | Adjunctive 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 |
| Hydroxyaldimines | Activity 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-367 | Exerted 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 infections | 25294047 |
| 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 fungicide | Targets the motor domain of type I myosin, specific to Fusarium | | Real-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 congeners | Congeners of KB425796-A, named KB425796-B, -C, -D, -E, -F, -G, -H, -I, -J and -K, which exhibited diverse antifungal potencies against A. fumigatus | | Identification 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 micafungin | Antifungal 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 hydrochloride | Wide 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 agent | The 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 Efinaconazole | Activity 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: PMC5655049 | 28848012 |
| Macrocyclic amidinoureas | Potent 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 |
| Magnolol | MIC?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 |
| ME1111 | MIC90 against dermatophyte strains was 0.25 micro g/ml, MFC90s against Trichophyton rubrum and Trichophyton mentagrophytes were 8 micro g/ml | | In 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 |
| ME1111 | ME1111 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 agent | Broad 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 acetophenone | Activity 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) derivatives | Antifungal 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 analogues | Bis-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 ketone | All 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-lysines | Inhibits 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 Activity | 27556953 |
| New series of thiazolyl-triazole Schiff bases B1-B15 | Potential 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) derivative | Activity 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 9139 | Activity 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 MMV687807 | The 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 W1 | PcPAF 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-118 | Inhibitor 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-743,872 | Activity 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 derivative | R-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/ml | | Antifungal 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 derivatives | Potent 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 triazole | Varied 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-078 | Potency 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 arylamidine | Activity 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 arylamidine | Potent 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-1161 | Trichophyton 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 fumigatus | | Chemosensitization prevents tolerance of Aspergillus fumigatus to antimycotic drugs | 18486603 |
| triazole derivatives containing substituted 1,2,3-triazole-piperdine side chains | The 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-1129 | MIC 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 MIC90values | | The 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-1129 | Promising 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 oxadiazole | Minimum 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 vivo | | Taken 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-Lactones | Broad spectrum of antifungal activity, including against resistant fungal species | Toxicity 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 MIC | Structure-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 1067 | ECQ 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 compounds | Furthermore, 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 dichloride | 1-(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 arylamidine | The 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 |
| Rezafungin | | | Rezafungin 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-yl | Mminimum 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/ml | Development of effective fungicides can not only provide new means for clinical treatment, but also reduce the occurrence of fungal resistance. | 33117733 |
| Aromatic-rich piperazines | Inhibit biofilm formation by C. albicans. | | Effective treatment of infectious diseases now requires new antimicrobial therapies. | 33091849 |
| Metyltetraprole | Activity against Z. tritici, P. teres, Ramularia collo-cygni, Pyrenophora tritici-repentis, and several other plant pathogenic fungi | | The 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)benzohydrazide | Compounds 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 strains | | In 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, PC1244 | PC1244 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 mutations | Compound 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 triazaacenaphthylene | Gepotidacin 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-Carbohydrazides | N | | Overall results suggest that these compounds have the potential to become promising antimicrobial drugs against MDR strains. | 36615406 |
| Efinaconazole, a novel triazole | Fusarium 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 Polylysines | hyperbranched 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 albicans | | hese 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, respectively | no 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 derivatives | The derivative compound B25 was found to have good synergistic effects with fluconazole against azole-resistant candidiasis | to avoid potential mammalian toxicity. | promising lead compound for drug discovery targeting fungal Hsp90 and deserves further investigation. | 36029272 |
| Non-Antibiotic Antimony-Based Antimicrobials | Antifungal effect of new tetraphenyl-antimony(V) cyanoximates determined using a disc-diffusion assay against selected two human fungal pathogens | | Antifungal 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 -quinazoline | The 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 7544. | an acceptable safety profile | With 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 derivatives | hese compounds prevented the growth of both fluconazole-susceptible and fluconazole-resistant Candida albicans and Candida auris strains. | | | 36403201 |
| novel indole and indoline derivatives | The results showed that title compounds exhibited good antifungal effect on Azole-resistant C. albicans | | inhibit 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)iron | The 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 derivatives | 3,4,5-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-tetrahydroquinoline | Commercially 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 fungi | | In 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) derivative | 7-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 albicans | | In 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 derivatives | two 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 enzyme | a 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 B | low 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 |
| baicalein | These 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 compound | Compared 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 activities | 36562209 |
| Lipid-Modified Chitin-Binding Domains | LysM-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 Derivatives | compound 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 (9a | The 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 resistance | 36570236 |
| chelerythrine combined with fluconazole | A 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 mefentrifluconazole | The results suggest that triazole resistance in A. fumigatus could be resulted from the selection of mefentrifluconazole at concentrations larger than 2 mg L-1 | | Mefentrifluconazole 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 olorofim | Effective against- Azole resistance in Aspergillus fumigatus | | The 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 Synthesis | Future 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 (Brij | control of C. auris infections and resistance as well as decrease the side effects of this drug | | NEA 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 fluconazole | Synergism 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-phenylacetamide | A1Cl 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 acid | boric acid inhibited C. albicans hyphal formation and reduced mature biofilm biomass and metabolic activity in all isolates in a dose-dependent manner | | Overall, 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 |
| Nitroxoline | MIC50/90 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 species | | The 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 isolates | | Juglone 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 fluconazole | against suspensions and biofilms of Candida auris | | Conclusion: 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 albicans | | Therefore, Hsp90/HDAC dual inhibitors represent a new strategy for the development of novel antifungal therapeutics to combat azole-resistant candidiasis. | 34742014 |
| Recombinant Myeloperoxidase | | | Taken 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 acid | All 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) complexes | potent agents against resistant Candida albicans | | This 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 Fluconazole | against Candida albicans via Inhibition of Adhesion and Yeast-To-Hypha Transition | | In 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 acid | against strains of Candida spp. resistant to fluconazole | | We 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-6 | the 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 deficiency | causes dramatic growth inhibition of the human fungal pathogens Aspergillus fumigatus, Candida albicans, and Cryptococcus neoformans | | Thus, 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 Molecules | Promising Inhibitors of Black Fungi and Pathogenic Bacteria | | Furthermore, 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 derivatives | antifungal 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 study | 34749201 |
| 3-thiophene derivatives | showed 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 Derivatives | Combination Treatment of Azole-Resistant Candidiasis | | These 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 2a11 | compound 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 hydrochloride | against fluconazole-resistant Candida albicans | | Conclusion. 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 Drugs | Restores Efficacy against Resistance Conferred by Mutated Glucan Synthase | | This 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 azoles | in 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 |
| olorofim | Inhibition of azole-resistant Aspergillus fumigatus biofilm at various formation stages | | Conclusions: 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 Alkaloids | Jervine 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-2 | Among 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 chelator | 19ak exhibits minimal cytotoxicity and potent activity against either azole-sensitive or azole-resistant fungal pathogens, inhibits fungal ribosome biogenesis mainly by disrupting intracellular zinc homeostasis | | This study provides the basis of thiosemicarbazone derivative 19ak as a metal chelator for the treatment of fungal infections. | 35412374 |
| BDDE-Inspired Chalcone Derivatives | chalcones 13 and 14 showed promising antifungal activity against the dermatophyte clinical strain of Trichophyton rubrum | | BDDE-Inspired Chalcone Derivatives to Fight Bacterial and Fungal Infections | 35621966 |
| sertraline with fluconazole | luconazole 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 incubation | | Conclusion: 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 antifungals | The 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 |
| benzbromarone | potential folate inhibitors of Candida albicans | | Based 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 |
| surfactin | exerted antifungal effect against Candida albicans | | Our 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 |
| octenidine | against emerging echinocandin-, azole- and multidrug-resistant Candida albicans and Candida glabrata | | Conclusion: 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 metabolites | All the diterpenes showed fungistatic effects (ranging from 19 | | Ent-hardwickiic acid from C. pubiflora and its microbial metabolites are more potent than fluconazole in vitro against Candida glabrata | 34995375 |
| adamantane derivatives | five 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 roxburghiana | For 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 hybrids | DPA-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 phosphatidylserine | | Conclusion: GA has potential antifungal activity against Candida spp. | 35354285 |
| indole and indoline derivatives | against Candida albicans as potent antifungal agents | | The 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 Derivatives | Compounds 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 Pyridine | as an Inhibitor of Candida albicans Erg11 | | This 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 saponin | In 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 albicans | 35552063 |
| Arylamidine T-2307 | the 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 line | these 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 derivatives | The 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 agents | 35932582 |
| Hydroxyethyl Naphthalimides | These 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 derivatives | MIC 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 method | 35716118 |
| 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 cells | | HAL-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 dumicola | The 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 defense | 36073497 |
