Preparation and evaluation of 3,4"-ester derivatives of 16-membered macrolide antibiotics related to tylosin.

Abstract
A large group of ester derivatives of tylosin-related macrolide was prepared in which the hydroxy groups at C-3 and C-4" were acylated by either chemical or biochemical methods. Most of the derivatives exhibited excellent in vitro antimicrobial activity. However, only the 3,4"-diacyl derivatives of tylosin and macrocin showed any significant im parameters of in vivo efficiency against experimental infections in rodents.

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