Preparation and evaluation of 3,4''-ester derivatives of 16-membered macrolide antibiotics related to tylosin.
A large group of ester derivatives of tylosin-related macrolides was prepared in which the hydroxyl 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 improvements of in vivo efficacy against experimental infections in rodents.
D000215:Acylation; D000900:Anti-Bacterial Agents / Q000096:biosynthesis / Q000138:chemical synthesis* / Q000494:pharmacology; D055598:Chemical Phenomena; D002621:Chemistry; D007933:Leucomycins / Q000096:biosynthesis / Q000138:chemical synthesis* / Q000494:pharmacology; D013302:Streptomyces / Q000378:metabolism*; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D007933:Leucomycins