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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Veröffentlicht in:Journal of medicinal chemistry 1993-10, Vol.36 (22), p.3219-3223
Hauptverfasser: Ternansky, Robert J, Draheim, Susan E
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container_title Journal of medicinal chemistry
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creator Ternansky, Robert J
Draheim, Susan E
description 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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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
title Structure-activity relationship within a series of pyrazolidinone antibacterial agents. 1. Effect of nuclear modification on in vitro activity
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