WATER-SOLUBLE PRADIMICIN DERIVATIVES, SYNTHESIS AND ANTIFUNGAL EVALUATION OF N,N-DIMETHYL PRADIMICINS

被引:36
作者
OKI, T
KAKUSHIMA, M
NISHIO, M
KAMEI, H
HIRANO, M
SAWADA, Y
KONISHI, M
机构
[1] Bristol-Myers Research Institute, Ltd., Tokyo Research Center, Tokyo 153, 2-9-3 Shimo-meguro, Meguro-ku
关键词
D O I
10.7164/antibiotics.43.1230
中图分类号
Q81 [生物工程学(生物技术)]; Q93 [微生物学];
学科分类号
071005 ; 0836 ; 090102 ; 100705 ;
摘要
Three N,N-dimethyl pradimicins were synthesized by reductive alkylation of pradimicins A, E and FA-2 and evaluated for antifungal activity, water solubility and acute toxicity in mice. They showed in vitro antifungal activity superior to pradimicin A. N,N-Dimethylpradimicins E and FA-2 showed great improvement in water solubility and animal tolerance. N,N-Dimethylpradimicin FA-2 was effective in 3 experimental in vivo fungal infection models. © 1990, JAPAN ANTIBIOTICS RESEARCH ASSOCIATION. All rights reserved.
引用
收藏
页码:1230 / 1235
页数:6
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