Synthesis and evaluation of 2 beta-oxyimino and alkenylpenicillanic acid sulfone derivatives as beta-lactamase inhibitors

Arch Pharm (Weinheim). 1999 Jan;332(1):7-12. doi: 10.1002/(sici)1521-4184(19991)332:1<7::aid-ardp7>3.0.co;2-m.

Abstract

The synthesis and in vitro synergies of 2 beta-alkenyl and oxyiminopenam sulfone derivatives are described. Most of the compounds synthesized exhibited good inhibitory activities and synergistic antibacterial activities with piperacillin and ceftriaxone, respectively, against several beta-lactamase producing strains. Particularly the 2 beta-alkenylpenam sulfone derivatives. 1e and 1g, showed good synergistic activity with ceftriaxone against Citrobacter freundi NIH 10018-68 and Proteus vulgaris 20. Also the compounds 2a, 2c, and 2f, 2 beta-oxyiminopenam sulfone derivatives, exhibited improved synergistic activity with piperacillin against Citrobacter freundi NIH 10018-68.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Ceftriaxone / pharmacology
  • Cephalosporins / pharmacology
  • Citrobacter freundii / drug effects
  • Drug Synergism
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / pharmacology
  • Microbial Sensitivity Tests
  • Penicillanic Acid / analogs & derivatives*
  • Penicillanic Acid / chemical synthesis*
  • Penicillanic Acid / pharmacology
  • Penicillins / pharmacology
  • Piperacillin / pharmacology
  • Sulfones / chemical synthesis*
  • Sulfones / pharmacology
  • beta-Lactamase Inhibitors*

Substances

  • Cephalosporins
  • Enzyme Inhibitors
  • Penicillins
  • Sulfones
  • beta-Lactamase Inhibitors
  • Ceftriaxone
  • Penicillanic Acid
  • Piperacillin