Synthesis and antibacterial activity of novel 6-O-substituted erythromycin A derivatives

A series of novel 6-O-substituted erythromycin A derivatives has been synthesized. Good in vitro antibacterial activity has been demonstrated for analogues incorporating a variety of structural features. The methodology disclosed is expected to find application in the design of future macrolide anti...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2000-04, Vol.10 (8), p.815-819
Main Authors: CLARK, R. F, ZHENKUN MA, YAT SUN OR, SANYI WANG, GRIESGRABER, G, TUFANO, M, HONG YONG, LEPING LI, XIAOLIN ZHANG, NILIUS, A. M, CHU, D. T. W
Format: Article
Language:English
Subjects:
Anti-Infective Agents - chemical synthesis
Anti-Infective Agents - pharmacology
Antibacterial agents
Antibiotics. Antiinfectious agents. Antiparasitic agents
Biological and medical sciences
Erythromycin - analogs & derivatives
Erythromycin - chemical synthesis
Erythromycin - pharmacology
Medical sciences
Microbial Sensitivity Tests
Pharmacology. Drug treatments
Structure-Activity Relationship
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Summary:A series of novel 6-O-substituted erythromycin A derivatives has been synthesized. Good in vitro antibacterial activity has been demonstrated for analogues incorporating a variety of structural features. The methodology disclosed is expected to find application in the design of future macrolide antibiotics that target the prevalent bacterial resistance problem.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(00)00106-2