Triazole Antifungals. IV. Synthesis and Antifungal Activities of 3-Acylamino-2-aryl-2-butanol Derivatives

Toshiyuki KONOSU; Yawara TAJIMA; Noriko TAKEDA; Takeo MIYAOKA; Mayumi KASAHARA; Hiroshi YASUDA; Sadao OIDA

doi:10.1248/cpb.39.2581

Toshiyuki KONOSU, Yawara TAJIMA, Noriko TAKEDA, Takeo MIYAOKA, Mayumi KASAHARA, Hiroshi YASUDA, Sadao OIDA

Author information

Keywords: antifungal activity, 1, 2, 4-triazole, 3-acylamino-2-aryl-1-(triazol-1-yl)-2-butanol, cytochrome P-450 inhibitor, structure-activity relationship, oral activity

JOURNAL FREE ACCESS

1991 Volume 39 Issue 10 Pages 2581-2589

DOI https://doi.org/10.1248/cpb.39.2581

Details

Abstract

New triazole compounds were designed and synthesized as potential inhibitors of the fungal cytochrome P-450 14α-demethylase. In testing for antifungal activity against a mouse systemic Candida albicans infection, (2R, 3R)-3-acylamino-2-aroyl-2-butanol derivatives III exhibited remarkably high efficacy after oral or parenteral administration. The structure-activity relationships of these amidoalcohols were evaluated.

Corresponding author

Register with J-STAGE for free!