Synthesis and biological evaluation of benzazepine oxazolidinone antibacterials

Novel benzazepine oxazolidinone antibacterials were synthesized and evaluated against clinically relevant susceptible and resistant organisms. The effect of ring nitrogen position and N-substitution on antibacterial activity is examined. Novel benzazepine oxazolidinones were synthesized as potential...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2003-12, Vol.13 (23), p.4197-4200
Main Authors: Johnson, Paul D., Aristoff, Paul A., Zurenko, Gary E., Schaadt, Ronda D., Yagi, Betty H., Ford, Charles W., Hamel, Judith C., Stapert, Douglas, Moerman, Judy K.
Format: Article
Language:English
Subjects:
Acetamides - pharmacology
Animals
Anti-Bacterial Agents - chemical synthesis
Anti-Bacterial Agents - chemistry
Anti-Bacterial Agents - pharmacology
Benzazepines - pharmacology
Gram-Negative Bacteria - drug effects
Gram-Positive Bacteria - drug effects
Linezolid
Mice
Microbial Sensitivity Tests
Oxazolidinones - chemical synthesis
Oxazolidinones - chemistry
Oxazolidinones - pharmacology
Structure-Activity Relationship
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Summary:Novel benzazepine oxazolidinone antibacterials were synthesized and evaluated against clinically relevant susceptible and resistant organisms. The effect of ring nitrogen position and N-substitution on antibacterial activity is examined. Novel benzazepine oxazolidinones were synthesized as potential antibacterial agents. Compounds 27 and 39 displayed in vitro Gram-positive antibacterial activity comparable to linezolid against clinically relevant organisms.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2003.07.017