Bioorg Med Chem Lett. 2009 Apr 1;19(7):2013-7. Epub 2009 Feb 12.

Amide analogs of antifungal dioxane-triazole derivatives: synthesis and in vitro activities.

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Medicinal Chemistry Research Laboratories II, Daiichi Sankyo Co., Ltd, 1-16-13, Kitakasai, Edogawa-ku, Tokyo 134-8630, Japan.

Abstract

A new series of triazole compounds possessing an amide-part were efficiently synthesized and their in vitro antifungal activities were investigated. The amide analogs showed excellent in vitro activity against Candida, Cryptococcus and Aspergillus species. The MICs of compound 23d against C. albicans ATCC24433, C. neoformans TIMM1855 and A. fumigatus ATCC26430 were 0.008, 0.031 and 0.031 microg/mL, respectively, (MICs of fluconazole: 0.5, >4 and >4 microg/mL; MICs of itraconazole: 0.125, 0.25, 0.25 microg/mL). Furthermore, compound 23d was stable under acidic conditions.

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