dl-灰黄霉素及其同系物的合成与抗真菌活性。III.

Syntheses and antifungal activity of dl-griseofulvin and its congeners. III.

作者信息

Takeuchi Y, Watanabe I, Misumi K, Irie M, Hirose Y, Hirata K, Yamato M, Harayama T

机构信息

Faculty of Pharmaceutical Sciences, Okayama University, Japan.

出版信息

Chem Pharm Bull (Tokyo). 1997 Dec;45(12):2011-5. doi: 10.1248/cpb.45.2011.

DOI:10.1248/cpb.45.2011

PMID:9433771

Abstract

Several congeners (1b-g), with novel substituents on the benzene ring of griseofulvin, were prepared by the application of a synthetic method developed by us. Antifungal activity of these congeners decreased in order of dl-griseofulvin (1a) = 1d > 1b, c >> 1e-f (inactive). The relationship between the antifungal activity and the position or kind of substituents on the benzene ring of griseofulvin is discussed.

摘要

通过应用我们开发的一种合成方法，制备了几种在灰黄霉素苯环上带有新型取代基的同系物（1b - g）。这些同系物的抗真菌活性按以下顺序降低：dl - 灰黄霉素（1a）= 1d > 1b、c >> 1e - f（无活性）。讨论了灰黄霉素苯环上取代基的位置或种类与抗真菌活性之间的关系。