Structure-activity relationship within a series of pyrazolidinone antibacterial agents. 1. Effect of nuclear modification on in vitro activity

The synthesis and biological evaluation of a series of pyrazolidinone-containing mono- and bicyclic compounds are described. The results of this investigation indicate that the [3.3.0] ring system bearing strongly electron-withdrawing groups in the 3-position provides the optimal arrangement for ant...

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Bibliographic Details
Published inJournal of medicinal chemistry Vol. 36; no. 22; pp. 3219 - 3223
Main Authors Ternansky, Robert J, Draheim, Susan E
Format Journal Article
LanguageEnglish
Published United States American Chemical Society 29.10.1993
Subjects
Anti-Infective Agents - chemical synthesis
Anti-Infective Agents - pharmacology
Bridged Bicyclo Compounds - chemical synthesis
Bridged Bicyclo Compounds - pharmacology
Bridged Bicyclo Compounds, Heterocyclic
Pyrazoles - chemical synthesis
Pyrazoles - pharmacology
Structure-Activity Relationship
Thiazoles - chemical synthesis
Thiazoles - pharmacology
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Summary:The synthesis and biological evaluation of a series of pyrazolidinone-containing mono- and bicyclic compounds are described. The results of this investigation indicate that the [3.3.0] ring system bearing strongly electron-withdrawing groups in the 3-position provides the optimal arrangement for antibacterial activity. Two highly potent derivatives, LY193239 and LY255262, have been selected for further preclinical evaluation.
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ISSN:0022-2623
1520-4804
DOI:10.1021/jm00074a001