6-Exomethylenepenam 유도체의 베타락타마제 효소억제력과 베타락탐항생제 병용시 활성비교

β-Lactamase Inhibitory Activity and Comparative Activity of 6-Exomethylenepenam Derivatives Combined with β-Lactam Antibiotics

In vitro β-lactamase inhibitory activity of 6-exomethylenepenam compounds (1,2,3,4 and 5) was compared with clavulanic acid, sulbactam and tazobactam. The inhibitory activity of compound 3 was stronger than those of sulbactam and clavulanic acid against Type I and II enzymes and stronger than tazobactam against Type III, IV, TEM enzymes. The inhibitory activity of 5 was stronger than sulbactam and clavulanic acid against Type I and II enzymes and stronger than tazobactam against Type III and IV enzymes. The in vitro antimicrobial activity of 3,4 and 5 combined with ampicillin and cefoperazone was compared with the sulbactam against β-lactamase producing 27 strains. But, synergistic activity of 3 and 5 was inferior to tazobactam.