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 [3.3.01 ring system bearing stron gly 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 ev aluation.