beta-Lactamase epidemiology and the utility of established and novel beta-lactamase inhibitors

Expert Opin Investig Drugs. 2000 Feb;9(2):247-61. doi: 10.1517/13543784.9.2.247.


beta-Lactamase inhibitor:beta-lactam combinations remain one of the most successful strategies for the treatment of bacterial infections. Over the last 20 years the number and diversity of serine and metallo active site beta-lactamases has increased dramatically. This review highlights some of the new additions to the beta-lactamase arena and discusses how the commercially available beta-lactamase inhibitors are keeping pace with the changing epidemiology of beta-lactamases. In addition, we survey the progress with the design of novel inhibitors of serine and metallo-beta-lactamases. Focus is given to the recent advances in the design of metallo-beta-lactamase inhibitors as these enzymes pose a serious emerging threat to the use of all beta-lactam based therapies.

Publication types

  • Review

MeSH terms

  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Anti-Bacterial Agents / therapeutic use
  • Bacterial Proteins*
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology
  • Humans
  • Structure-Activity Relationship
  • beta-Lactamase Inhibitors
  • beta-Lactamases* / classification
  • beta-Lactams


  • Anti-Bacterial Agents
  • Bacterial Proteins
  • Enzyme Inhibitors
  • beta-Lactamase Inhibitors
  • beta-Lactams
  • beta-lactamase IMP-1
  • beta-lactamase PIT-2
  • beta-Lactamases
  • beta-lactamase TEM-1