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 antibacterial activity. Two highly potent derivatives, LY193239 and LY255262, have been selected for further preclinical evaluation.
Ternansky
R J
RJ
Lilly Research Laboratories, Eli Lilly and Co., Indianapolis, Indiana 46285.
Draheim
S E
SE
D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D001643:Bridged Bicyclo Compounds / Q000138:chemical synthesis / Q000494:pharmacology; D019086:Bridged Bicyclo Compounds, Heterocyclic; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis* / Q000494:pharmacology*
D000890:Anti-Infective Agents; D001643:Bridged Bicyclo Compounds; D019086:Bridged Bicyclo Compounds, Heterocyclic; D011720:Pyrazoles; D013844:Thiazoles; C084126:LY 255262; C068345:LY 193239