Structure-activity Relationships of Biphenyl Tetrazoles as Metallo-Beta-Lactamase Inhibitors

Bioorg Med Chem Lett. 1999 Sep 20;9(18):2741-6. doi: 10.1016/s0960-894x(99)00458-8.

Abstract

Resistance to carbapenem antibiotics in gram-negative bacteria is due, in part, to expression of a wide spectrum metallo-beta-lactamase, which renders the drug inactive. Biphenyl tetrazoles containing 3-n-butyl-1-phenylpyrazole-5-carboxylates or the corresponding 5-ethyl esters were found to inhibit metallo-beta-lactamases as well as renal dehydropeptidase I to a lesser extent.

MeSH terms

  • Bacteroides fragilis / enzymology
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / pharmacology*
  • Structure-Activity Relationship
  • Tetrazoles / chemistry*
  • Tetrazoles / pharmacology*
  • beta-Lactamase Inhibitors*

Substances

  • Enzyme Inhibitors
  • Tetrazoles
  • beta-Lactamase Inhibitors