6위치 엑소 메칠렌 치환 페남계 베타락타마제 억제제의 베타락탐항생제와 병용시 활성비교(I)

Comparison of the Activities of Novel beta-Lactamase Inhibitors, 6-Exomethylene Penamsulfones, with Other beta-Lactamase Inhibitors as Combined with beta-Lactam Antibiotics (I)

In this approach, the antimicrobial activities of the compounds were compared with the beta-lactam antibiotics against beta-lactamase producing strains in vitro. Heterocyclyl exomethylenepenam derivatives were several numbers of 6-exomethylenepenam sodiums (CH1240, CH1245, CH1250, CH2140, CH2145, CH2150). The inhibitory concentraion assay of six compounds were compared with clavulanic acid, sulbactam, tazobactam. Clavulanic acid, sulbactam and tazobactam are used as inhibitors of a variety of plasmid-mediated beta-lactamases. In vitro beta-lactamase inhibitory assay, CH1240 and CH2140 were more active than clavulanic acid, sulbactam and tazobactam against beta-lactamases overally. And in vitro comparative antimicrobial susceptibility test of six inhibitors were performed with mixed forms of ampicillin, cefotaxime, amoxicillin, ticarcillin, piperacillin, cefoperazone against beta-lactamase producing 31 species strains. Consequently CH2140 and CH1240 among the six compounds enhanced the activity of the beta-lactams for 31 beta-lactamase producing strains.