Design, synthesis and bioactivity evaluation of tribactam beta lactamase inhibitors

Bioorg Med Chem Lett. 2002 Mar 25;12(6):971-5. doi: 10.1016/s0960-894x(02)00061-6.

Abstract

Known carbapenem compounds with inhibitory effect towards beta-lactamase enzymes are formed from bicyclical beta lactam structural scaffolds. On the basis of results from theoretical computational methods and molecular modelling we have designed and developed a synthetic route towards novel, biologically active tricyclic derivatives of carbapenems.

MeSH terms

  • Bacillus cereus / enzymology
  • Carbapenems / chemical synthesis*
  • Carbapenems / pharmacology
  • Dose-Response Relationship, Drug
  • Drug Design
  • Hydrolysis / drug effects
  • Models, Molecular
  • beta-Lactamase Inhibitors*
  • beta-Lactams / metabolism

Substances

  • Carbapenems
  • beta-Lactamase Inhibitors
  • beta-Lactams