6-트리아졸 엑소메칠렌펜남 유도체의 베타락타마제 효소억제력과 베타락탐항생제 병용시 활성비교

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

In vitro β-lactamase inhibitory activity of 6-triazole exomethylenepenam compounds (1,2,3,4,5 and 6) was compared with clavulanic acid, sulbactam and tazobactam. The inhibitory activity of 3, 4 and 5 was stronger than those of sulbactam, clavulanic acid and tazobactam against Type Ⅳ enzymes. And, inhibitory activity of 3 and 4 was stronger than those of sulbactam, clavulanic acid and tazobactam against Type Ⅲ enzymes. The in vitro antimicrobial activity of 3, 4 and 5 combined with ampicillin was better than those with sulbactam and with cefoperazone was compared with the sulbactam against β-lactamase producing 27 strains. The synergistic activity of (Z)-form compounds (3 and 5) was better than that of (E)-form compound (4) and sulfone compound (5) was better than sulfide compound (3).