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Novel Triazole Alcohol Antifungals Derived From Fluconazole: Design, Synthesis, and Biological Activity Publisher Pubmed



Hashemi SM1 ; Badali H2 ; Faramarzi MA3 ; Samadi N4 ; Afsarian MH2, 6 ; Irannejad H5 ; Emami S5
Authors

Source: Molecular Diversity Published:2015


Abstract

A series of new triazole alcohol antifungals were designed by replacing one of the triazolyl moiety from fluconazole with a distinct 4-amino-3-mercapto-1,2,4-triazole motif, which is found in some antimicrobial agents. The antimicrobial susceptibility testing of target compounds demonstrated that the direct analogs of fluconazole (difluorophenethyl-triazoles) were less active against fungi, while compound 10h containing dichloro substitutions on both phenyl rings of the molecule had potent activity against yeasts including Candida albicans (four strains) and Cryptococcus neoformans (MICs = 2–8 μg/mL). Also, compound 10h was active against Candida parapsilosis, Epidermophyton floccosum, and Trichophyton mentagrophytes, while it showed no activity against Gram-positive and Gram-negative bacteria. Finally, a molecular docking study suggested that compound 10h interacts suitably with lanosterol 14α-demethylase, which is the key enzyme in ergosterol biosynthesis. © 2014, Springer International Publishing Switzerland.
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