Synthesis and biological evaluation of novel triazole derivatives as antifungal agents

A series of 1-(benzylamino)-2-(2,4-difluorophenyl)-3-(1H-1,2,4-triazol-1-yl)propan-2-ols compounds were synthesized and evaluated for their antifungal activities in vitro. The results showed that compounds 6A and 6B exhibited good antifungal activity. Compound 6A8 showed the strongest antifungal activity, which was significantly higher than that of the lead compounds and positive-control drugs Fluconazole and Itraconazole. In particular, the antifungal activity of compound 6A8 against Candida albicans and Candida krusei (MIC80 both at 0.00097 μg/mL) was 515 and 64 times that of Fluconazole, respectively. The structure–activity relationships of the synthesized compounds were discussed, and the docking model of the target compounds with fungal lanosterol 14α-demethylase (CYP51) was analyzed.

A series of triazle compounds with different nitrogen substitutions were synthesized. Compound 6A8 showed the strongest antifungal activity.Figure optionsDownload as PowerPoint slide