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[ ${\beta}$ ]-Lactamase Inhibitory Activity and Comparative Activity of 6-Triazole Exomethylenepenam Derivatives Combined with ${\beta}$-Lactam Antibiotics  

Im Chaeuk (Division of Medicinal Chemistry, College of Pharmacy, Chung-ang University)
Oh Jung Suk (Division of Medicinal Chemistry, College of Pharmacy, Chung-ang University)
Lee Sun Hye (Division of Medicinal Chemistry, College of Pharmacy, Chung-ang University)
Kim Kyoung Won (Division of Medicinal Chemistry, College of Pharmacy, Chung-ang University)
Yim Chul Bu (Division of Medicinal Chemistry, College of Pharmacy, Chung-ang University)
Publication Information
YAKHAK HOEJI / v.49, no.1, 2005 , pp. 51-55 More about this Journal
Abstract
In vitro ${\beta}$-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 ${\beta}$-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).
Keywords
antimicrobial activity; 6-exomethylenepenam;
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