title: Triazole antifungals. IV. Synthesis and antifungal activities of 3-acylamino-2-aryl-2-butanol derivatives.
abstract: New triazole compounds were designed and synthesized as potential inhibitors of the fungal cytochrome P-450 14 alpha-demethylase. In testing for antifungal activity against a mouse systemic Candida albicans infection, (2R,3R)-3-acylamino-2-aryl-2-butanol derivatives III exhibited remarkably high efficacy after oral or parenteral administration. The structure-activity relationships of these amidoalcohols were evaluated.
authors.affiliation: Medicinal Chemistry Research Laboratories, Sankyo Co., Ltd., Tokyo, Japan.
authors.forename: T
authors.initials: T
authors.lastname: Konosu
authors.forename: Y
authors.initials: Y
authors.lastname: Tajima
authors.forename: N
authors.initials: N
authors.lastname: Takeda
authors.forename: T
authors.initials: T
authors.lastname: Miyaoka
authors.forename: M
authors.initials: M
authors.lastname: Kasahara
authors.forename: H
authors.initials: H
authors.lastname: Yasuda
authors.forename: S
authors.initials: S
authors.lastname: Oida
mesh_terms: D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002176:Candida albicans / Q000187:drug effects / Q000201:enzymology; D065607:Cytochrome P-450 Enzyme Inhibitors; D010088:Oxidoreductases / Q000037:antagonists & inhibitors; D058886:Sterol 14-Demethylase; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000935:Antifungal Agents; D065607:Cytochrome P-450 Enzyme Inhibitors; D014230:Triazoles; D010088:Oxidoreductases; C548415:Cyp51 protein, mouse; D058886:Sterol 14-Demethylase