Biomolecules & Therapeutics

The Korean Society of Applied Pharmacology (한국응용약물학회)
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[ β ]-Lactamase Inhibitory Activities of New 6-tricyclic Substituted Exomethylene Penam Sulfones

  • Lee, Su-Jin (School of Pharmacy, Ewha Womans University) ;
  • Kim, Hyun-Jin (School of Pharmacy, Ewha Womans University) ;
  • Sheen Yhun Y. (School of Pharmacy, Ewha Womans University) ;
  • Lee, Kwan-Soon (Hanmi Research Center) ;
  • ParkChoo, Hea-Young (School of Pharmacy, Ewha Womans University)
  • Published : 2006.12.30
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Abstract

Derivatives of penicillanic acid sulfones are known to be irreversible inhibitors of $\beta$-lactamase. Eight 6-tricyclic methylene penicillanic acid sulfones were prepared, and their $\beta$-lactamase inhibitory activities were evaluated against $\beta$-lactamase types I, II, III and IV. Among the tricycles attached to 6-exomethylenepenam sulfones, thiazolobenzimidazole(12a-12b), fluorene(12c), and carbazole(12e), showed inhibitory activity on type I, II and III $\beta$-lactamase. But phenanthrene(12d), and anthracene(12f-12h) derivatives showed little $\beta$-lactamase inhibitory activity. The synergic effects of the selected compound(l2b) in 1:4 combination with piperacillin showed some protection to piperacillin for the resistant strains of E. coli DC2 and P. aeruginosa 1771.

Keywords

References

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