Synthesis and SAR studies of biaryloxy-substituted triazoles as antifungal agents

A series of 1-(substituted biaryloxy)-2-(2,4-difluorophenyl)-3-(1H-1,2,4-triazol-1-yl) propan-2-ol were synthesized and their antifungal activities were evaluated against eight human pathogenic fungi in vitro. Seventeen compounds showed activity 4- to 64-fold higher than voriconazole against Candida albicans. SAR clearly suggested that introduction of a biaryloxy side chain greatly enhanced the antifungal activity of triazole analogs against Candida species.

Graphical abstractA series of novel biaryloxy-substituted triazole derivatives were synthesized and evaluated for their antifungal activity against eight human pathogenic fungi in vitro. Seventeen compounds showed higher activity than voriconazole against Candida albicans.Figure optionsDownload full-size imageDownload as PowerPoint slide