Design and synthesis of novel inhibitors of gelatinase B

Bioorg Med Chem Lett. 2002 Aug 19;12(16):2201-4. doi: 10.1016/s0960-894x(02)00365-7.

Abstract

A new method was developed to identify nonpeptidic metalloproteinase inhibitors with novel zinc binding groups. Application of this method to matrix metalloproteinase-9 resulted in the identification of aminomethyl benzimidazole analogue 7a with an IC(50)=13 microM.

Publication types

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

MeSH terms

  • Benzimidazoles / chemical synthesis*
  • Benzimidazoles / chemistry
  • Benzimidazoles / metabolism
  • Benzimidazoles / pharmacology*
  • Binding Sites
  • Drug Design*
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / metabolism
  • Enzyme Inhibitors / pharmacology*
  • Inhibitory Concentration 50
  • Matrix Metalloproteinase Inhibitors*
  • Molecular Structure
  • Solubility
  • Zinc / metabolism

Substances

  • Benzimidazoles
  • Enzyme Inhibitors
  • Matrix Metalloproteinase Inhibitors
  • Zinc