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 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.

• Authors: H A Kirst, M Debono, K E Willard, B A Truedell, J E Toth, J R Turner, D R Berry, B B Briggs, D S Fukuda, V M Daupert
• Journal: The Journal of antibiotics (J Antibiot (Tokyo)) Vol. 39 Issue 12 Pg. 1724-35 (Dec 1986) ISSN: 0021-8820 [Print] England
• PMID: 3818446 (Publication Type: Journal Article)

Chemical References

• Anti-Bacterial Agents
• Leucomycins

Topics

• Acylation
• Anti-Bacterial Agents (biosynthesis, chemical synthesis, pharmacology)
• Chemical Phenomena
• Chemistry
• Leucomycins (biosynthesis, chemical synthesis, pharmacology)
• Streptomyces (metabolism)
• Structure-Activity Relationship