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

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

  • J Med Chem. 1993 Oct 29;36(22):3219-23. doi: 10.1021/jm00074a001.
R J Ternansky 1,  S E Draheim
Affiliations

Affiliation

  • 1 Lilly Research Laboratories, Eli Lilly and Co., Indianapolis, Indiana 46285.
PMID: 8230111 DOI: 10.1021/jm00074a001
Abstract

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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