Design, synthesis, and evaluation of a pyrrolinone-based matrix metalloprotease inhibitor

Org Lett. 2000 Nov 30;2(24):3809-12. doi: 10.1021/ol000254p.

Abstract

[reaction: see text] A pyrrolinone-based hydroxamate matrix metalloprotease inhibitor, (-)-1, has been designed and synthesized. Enzymatic assay revealed that (-)-1 inhibited three of the ten matrix metalloprotease enzymes examined and as such represents a new, potentially important lead structure.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Aldehydes
  • Drug Design
  • Isoenzymes / antagonists & inhibitors
  • Metalloendopeptidases / antagonists & inhibitors*
  • Metalloendopeptidases / chemistry
  • Models, Molecular
  • Protease Inhibitors / chemical synthesis*
  • Protease Inhibitors / chemistry
  • Pyrroles / chemical synthesis*
  • Pyrroles / chemistry

Substances

  • Aldehydes
  • Isoenzymes
  • Protease Inhibitors
  • Pyrroles
  • Metalloendopeptidases