Matsubara H, Inokoshi J, Nakagawa A, Tanaka H, Omura S
J Antibiot (Tokyo). 1983 Dec;36(12):1713-21. doi: 10.7164/antibiotics.36.1713.
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.
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。