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.

A 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 as PowerPoint slide