Triazole antifungals. IV. Synthesis and antifungal activities of 3-acylamino-2-aryl-2-butanol derivatives.
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.
Konosu
T
T
Medicinal Chemistry Research Laboratories, Sankyo Co., Ltd., Tokyo, Japan.
Tajima
Y
Y
Takeda
N
N
Miyaoka
T
T
Kasahara
M
M
Yasuda
H
H
Oida
S
S
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
D000935:Antifungal Agents; D065607:Cytochrome P-450 Enzyme Inhibitors; D014230:Triazoles; D010088:Oxidoreductases; C548415:Cyp51 protein, mouse; D058886:Sterol 14-Demethylase