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泰乐菌素的化学修饰:泰乐菌素及去碳霉糖泰乐菌素C-20位氨基衍生物的合成。

Chemical modification of tylosin: synthesis of amino derivatives at C-20 position of tylosin and demycarosyltylosin.

作者信息

Matsubara H, Inokoshi J, Nakagawa A, Tanaka H, Omura S

出版信息

J Antibiot (Tokyo). 1983 Dec;36(12):1713-21. doi: 10.7164/antibiotics.36.1713.

DOI:10.7164/antibiotics.36.1713
PMID:6662813
Abstract

Reductive aminations of the aldehyde group at C-20 position of tylosin and demycarosyltylosin (desmycosin) were carried out using primary and secondary amines in the presence of sodium cyanoborohydride. Some of these derivatives brought about higher antimicrobial and ribosome-binding activities, and the structure-activity relationship is discussed.

摘要

在氰基硼氢化钠存在下,使用伯胺和仲胺对泰乐菌素和去碳霉糖泰乐菌素(地美霉毒)C-20位的醛基进行还原胺化反应。对其中一些衍生物的抗菌活性和核糖体结合活性进行了研究,并讨论了构效关系。

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