YAKHAK HOEJI (약학회지)

The Pharmaceutical Society of Korea (대한약학회)
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$\beta$-Lactamase Inhibitory Activity and Comparative Activity of Sulbactam Derivatives Combined with $\beta$-Lactam Antibiotics

Sulbactam 유도체의 베타락타마제 효소억제력과 베타락탐항생제 병용시 활성비교

  • 임채욱 (중앙대학교 약학대학 의약품화학 교실) ;
  • 박희석 (중앙대학교 약학대학 의약품화학 교실) ;
  • 김용현 (중앙대학교 약학대학 의약품화학 교실) ;
  • 임철부 (중앙대학교 약학대학 의약품화학 교실)
  • Published : 2002.12.01
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Abstract

In vitro $\beta$-lactamase inhibitory activity of 6-exomethylene sulbactam compounds (CH-120, 130, 140, 145, 150, 155) was compared with clavulanic acid, sulbactam and tazobactam. The inhibitory activity of CH-140 was stronger than sulbactam and clavulanic acid against Type II, III, IV, TEM enzymes and stronger than tazobactam against Type IV enzyme. The inhibitory activity of CH-145 was stronger than sulbactam and clavulanic acid against Type I, II, III, IV, TEM enzymes and stronger than tazobactam against Type III, IV enzymes. The in vitro antimicrobial activity of CH-140 and CH-145 combined with piperacillin and ceftriaxone was compared with the sulbactam and tazobactam against $\beta$-lactamase producing 31 strains. But, synergistic activity of CH-140 and CH-145 was inferior to tazobactam.

Keywords

References

  1. Sandanayaka, V. P., Prashad, A. S. : Resistance to $\beta$-lactarn antibiotics: Structure and mechanism based design of $\beta$-lactamase inhibitors. Current Medicinal Chemistry 9, 12, 1145 (2002)
  2. Jacoby, G. A., Archer, G. L. : New mechanisms of bacterial resistance to antimicrobial agents. New Eng. J Med. 324, 60, 1 (1991)
  3. Moland, E. S., Black, J. A., Ourada, J., Reisbig, M. D., Hanson, N. D., Thomson, K. S. : Occurrence of newer $\beta$-lactamases in Klebsiella pneumoniae isolates from 24 U.S. Hospitals. Antimicrobial Agents and Chemotherapy 46, 12, 3837 (2002)
  4. Laura, J. V., Piddock, Yu Fang Jin, Turner, H. L. : Activity of 13 $\beta$-lactam agents combined with BRL 42715 against $\beta$-lactamase producing Gram-negative bacteria compared to combinations with clavulanic acid, tazobactam and sulbactam. J. Antimicrob. Chemother. 31, 89 (1993) https://doi.org/10.1093/jac/31.1.89
  5. Smith, J. T., Hamilton-Miller, J. M. T., Knox, R. : Bacterial resistance to penicillins and cephalosporins. J. Pharm. Pharmac. 21, 337 (1969)
  6. Quinn, J. P. : Clinical significance of extended spectrum betalactamases. Eur. J. Clin. Microbiol. Infect. Dis. 13, (Suppl, 1), S39 (1994)
  7. Aconoff, S. C., Jacobs, M. R., Johenning, S., Yamabe, S. : Comparative activities of the -lactamase inhibitors YTR830, sodium clavulanate, and sulbactam combined with amoxicillin or ampicillin. J. Antimicrob. Chemother. 26, 580 (1984)
  8. Fassand, J. R., Prior, B. R. : Comparative In vitro activities of pperacillin-tazobactam and ticarcillin-clavulanate. Antimicrob. Agents Chemother. 33, 1268 (1989)
  9. Bennet, I., Broom, N. J. P., Bruton, G. S., Alvert, C., Clarke, B. P. Coleman, K., Edmondson, R., Edwards, P., Jones, D., Csbone, N. F., Walker, G. : 6-(Substituted methylene)penems, potent broad spectrum inhibitors of bacterial $\beta$-lactamase. J. Antibiotics 44, 331 (1990)
  10. Lin, Y. I., Bitha, P., Li, Z., Francisco, G. D. : Preparation of 3,6-disubstituted penam sulfone derivatives with $\beta$-lactamase inhibiting activity for use as antibacterial agents, US Patent 6395726 B1 20020528 (2002)
  11. Sandanayaka, V. P., Prashad, A. S. : Preparation of 6-(spirocyclopropyl) penicillanic acid 4,4-dioxides as $\beta$-lactamase inhibitors. U.S. Pat. Appl. 2002147178 A1 20021010 (2002)
  12. Waley, S. G. : A spectrophotometric assay of $\beta$-lactamase action on penicillins. Biochem. J. 139, 789 (1974)
  13. Ross, G. W., Chanter, K. V., Harris, A. M., Kirby, S. M., Marshall, M. J., O'Callaghan, C. H. : Comparison of assay techniques for $\beta$-lactamase activity. Anal. Biochem. 54, 9 (1973). https://doi.org/10.1016/0003-2697(73)90241-8
  14. American national standards institute : Methods for Dilution Antimicrobial Susceptibility Tests for Bacteria that grow Aerobically. 2nd. NCCLS Document M7-A2. 10, 1 (1990)