Chemical modification of tylosin: Synthesis of amino derivatives at c-20 position of tylosin and demycarosyltylosin

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. © 1983, JAPAN ANTIBIOTICS RESEARCH ASSOCIATION. All rights reserved.