வேதியியல் அறிவியல் இதழ்

Identification of Amino Acid Tethered Triazoles as Potential Antifungal Leads: Appraisal of their Mode of Action

Abstract

Parteek Prasher

A new set of compounds containing indole nucleus appended with carefully selected amino acids via a triazole linker are identified. These compounds showed substantial antifungal activities against the BWP17 strain of candida albicans. The preliminary screening of the compounds was done by docking in the active site of lanosterol 14-α demethylase enzyme (pdb ID - 3JUS) with ArgusLab.exe software. Subsequently the screened compounds were subjected to in-vivo antifungal assays. The probable mechanism of action of the test compounds was studied by GC analysis of the membrane metabolites. The compounds with tryptophan and histidine substitution were found to be most effective with MIC80 of 50.2 μg/ml and 78.81 μg/ml respectively. In the fungal cells treated with compound 3b the lanosterol levels were found to increase indicating that lanosterol 14-α demethylase enzyme could be the probable target. Additionally, the R6G influx/efflux assay provided the evidence for the fungicidal properties of the test compounds.