Carbon analogs of antifungal dioxane-triazole derivatives: Synthesis and in vitro activities

A new series of triazole compounds possessing a carbon atom in place of a sulfur atom were efficiently synthesized and their in vitro antifungal activities were investigated. The carbon analogs showed excellent in vitro activity against Candida, Cryptococcus, and Aspergillus species. The MICs of compound 1c against C. albicans ATCC24433, C. neoformans TIMM1855, and A. fumigatus ATCC26430 were 0.016, 0.016, and 0.125 μg/mL, respectively (MICs of fluconazole: 0.5, >4, and >4 μg/mL; MICs of itraconazole: 0.125, 0.25, and 0.25 μg/mL).

Stereoselective synthesis and in vitro antifungal activities of a novel series of triazole antifungal agents wherein the sulfur atom was replaced by a carbon atom are described.Figure optionsDownload as PowerPoint slide