Synthesis and Evaluation of New 1,3,4-Thiadiazole Derivatives as Potent Antifungal Agents.

ABSTRACT: With the goal of obtaining a novel bioactive compound with significant antifungal activity, a series of 1,3,4-thiadiazole derivatives (3a⁻3l) were synthesized and characterized. Due to thione-thiol tautomerism in the intermediate compound 2, type of substitution reaction in the final step was determined by two-dimensional (2D) NMR. In vitro antifungal activity of the synthesized compounds was evaluated against eight Candida species. The active compounds 3k and 3l displayed very notable antifungal effects. The probable mechanisms of action of active compounds were investigated using an ergosterol quantification assay. Docking studies on 14-α-sterol demethylase enzyme were also performed to investigate the inhibition potency of compounds on ergostero

SUBMITTER: Karaburun AC 

PROVIDER: S-EPMC6321371 | biostudies-literature | 2018 Nov

REPOSITORIES: biostudies-literature