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${\beta}-Lactamase$ Inhibitory Activity and Comparative Activity of 6-Benzothiazole Penicillin Derivatives in Combination with ${\beta}-Lactam$ Antibiotics  

Yoon, Sang-Bae (Division of Medicinal Chemistry, College of Pharmacy, Chung-ang University)
Im, Chae-Uk (Division of Medicinal Chemistry, College of Pharmacy, Chung-ang University)
Publication Information
YAKHAK HOEJI / v.52, no.4, 2008 , pp. 306-310 More about this Journal
Abstract
In vitro ${\beta}-lactamase$ 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 andsimilar to tazobactam against ${\beta}-lactamase$ 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 ${\beta}-lactamase$ 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 ${\beta}-lactamase$ producing strains, but it was inferior to tazobactam.
Keywords
antimicrobial activity${\beta}-lactamase$ inhibitors; 6-exomethylenepenam;
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