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螺旋霉素的化学修饰。II. 新螺旋霉素I的4'-脱氧衍生物及其12-(Z)-异构体的合成与抗菌活性

Chemical modification of spiramycins. II. Synthesis and antimicrobial activity of 4'-deoxy derivatives of neospiramycin I and their 12-(Z)-isomers.

作者信息

Sano H, Inoue M, Omura S

出版信息

J Antibiot (Tokyo). 1984 Jul;37(7):738-49. doi: 10.7164/antibiotics.37.738.

Abstract

4'-Deoxy derivatives of neospiramycin I and their 12-(Z)-isomers were synthesized by reductive dechlorination via 4'-epi-chloro derivatives. The 12-(Z)-derivatives were more active against bacteria in vitro than the corresponding 12-(E)-derivatives in spite of their low affinities to ribosomes.

摘要

通过4'-表氯衍生物的还原脱氯反应合成了新螺旋霉素I的4'-脱氧衍生物及其12-(Z)-异构体。尽管12-(Z)-衍生物对核糖体的亲和力较低,但它们在体外对细菌的活性比相应的12-(E)-衍生物更高。

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