Amide analogs of antifungal dioxane-triazole derivatives: synthesis and in vitro activities.
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.
Uchida
Takuya
T
Medicinal Chemistry Research Laboratories II, Daiichi Sankyo Co., Ltd, 1-16-13, Kitakasai, Edogawa-ku, Tokyo 134-8630, Japan.
Kagoshima
Yoshiko
Y
Konosu
Toshiyuki
T
D000577:Amides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001549:Benzamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002175:Candida / Q000187:drug effects; D004146:Dioxanes / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D014230:Triazoles / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology
D000577:Amides; D000935:Antifungal Agents; D001549:Benzamides; D004146:Dioxanes; D014230:Triazoles