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KMID : 0370220080520040306
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Yakhak Hoeji
2008 Volume.52 No. 4 p.306 ~ p.310
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β-Lactamase Inhibitory Activity and Comparative Activity of 6-Benzothiazole Penicillin Derivatives in Combination with β-Lactam Antibiotics
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Yoon Sang-Bae
Im Chae-Uk
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Abstract
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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.
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KEYWORD
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antimicrobial activity, ??-lactamase inhibitors, 6-exomethylenepenam
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