Synthesis and antifungal activities of (2R, 3R)-2-aryl-1-azolyl-3-(substituted amino)-2-butanol derivatives as topical antifungal agents.

H Ogura, H Kobayashi, K Nagai, T Nishida…

Index: Ogura, Hironobu; Kobayashi, Haruhito; Nagai, Kiyoshi; Nishida, Tokiko; Naito, Takanobu; Tatsumi, Yoshiyuki; Yokoo, Mamoru; Arika, Tadashi Chemical and Pharmaceutical Bulletin, 1999 , vol. 47, # 10 p. 1417 - 1425

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Citation Number: 21

Abstract

2-Aryl-1-azolyl-3-(substituted amino)-2-butanol derivatives I were prepared by ring-opening reaction of epoxides II with excess amine, and their antifungal activities were evaluated as topical agents. Azolyl-cyclic amine derivatives with a methylene group showed extremely strong activity with a broad spectrum in vitro. In general, anti-Trichophyton mentagrophytes activities of most of the topical antifungal agents are substantially reduced by addition of ...