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.