普拉地米星A衍生物丙氨酸部分修饰的合成及其抗真菌活性

Synthesis and antifungal activities of pradimicin A derivatives modification of the alanine moiety.

作者信息

Nishio M, Ohkuma H, Kakushima M, Ohta S, Iimura S, Hirano M, Konishi M, Oki T

机构信息

Bristol-Myers Squibb Research Institute, Tokyo, Japan.

出版信息

J Antibiot (Tokyo). 1993 Mar;46(3):494-9. doi: 10.7164/antibiotics.46.494.

DOI:10.7164/antibiotics.46.494

PMID:8478267

Abstract

Chemical modifications of the carboxyl group in the alanine moiety of pradimicin A were performed and in vitro and in vivo antifungal activities of the derivatives were examined in comparison with those of pradimicin A. The amide derivatives showed activities comparable to pradimicin A, indicating that the free carboxyl group can be modified without impairing the antifungal activity.

摘要

对普拉地米星A丙氨酸部分的羧基进行了化学修饰，并与普拉地米星A相比，检测了衍生物的体外和体内抗真菌活性。酰胺衍生物显示出与普拉地米星A相当的活性，这表明游离羧基可以被修饰而不损害抗真菌活性。