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

6-트리아졸 엑소메칠렌펜남 유도체의 베타락타마제 효소억제력과 베타락탐항생제 병용시 활성비교

  • 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)
  • 임채욱 (중앙대학교 약학대학 의약품화학 교실) ;
  • 오정석 (중앙대학교 약학대학 의약품화학 교실) ;
  • 이선혜 (중앙대학교 약학대학 의약품화학 교실) ;
  • 김경원 (중앙대학교 약학대학 의약품화학 교실) ;
  • 임철부 (중앙대학교 약학대학 의약품화학 교실)
  • Published : 2005.02.01

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

References

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