6-벤조치아졸 페니실린 유도체의 베타락타마제 효소억제력과 베타락탐항생제 병용시 활성비교

β-Lactamase Inhibitory Activity and Comparative Activity of 6-Benzothiazole Penicillin Derivatives in Combination with β-Lactam Antibiotics

In vitro β-lactamase inhibitory activity of 6-benzothiazole penicillins (1, 2, 3 and 4) was compared with clavulanic acid, sulbactam and tazobactam. The inhibitory activity of exomethylene compounds (3 and 4) was stronger than those of non-exomethylene compounds (1 and 2). The sulfide 3 showed stronger inhibitory activity than sulbactam, clavulanic acid and similar to tazobactam against β-lactamase Type I enzymes. The inhibitory activity of 4 was stronger than those of sulbactam, clavulanic acid and tazobactam against Type III and IV enzymes. The in vitro antimicrobial activity of ampicillin or cefoperazone combined with 3 or 4 was stronger than those of ampicillin or cefoperazone alone against many β-lactamase producing strains to show that compounds 3 and 4 have some synergistic effect. The synergistic activity of 3 and 4 was comparable to sulbactam in some β-lactamase producing strains, but it was inferior to tazobactam.