Dipeptidyl nitrile inhibitors of Cathepsin L

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4280-3. doi: 10.1016/j.bmcl.2009.05.071. Epub 2009 May 27.

Abstract

A series of potent Cathepsin L inhibitors with good selectivity with respect to other cysteine Cathepsins is described and SAR is discussed with reference to the crystal structure of a protein-ligand complex.

MeSH terms

  • Animals
  • Cartilage, Articular / pathology
  • Catalysis
  • Cathepsin L / antagonists & inhibitors*
  • Cathepsin L / chemistry*
  • Chemistry, Pharmaceutical / methods
  • Crystallography, X-Ray / methods
  • Drug Design
  • Humans
  • Ligands
  • Mice
  • Mice, Transgenic
  • Nitriles / chemical synthesis*
  • Nitriles / chemistry
  • Nitriles / pharmacology
  • Peptides / chemical synthesis
  • Peptides / pharmacology
  • Proteins / chemistry
  • Structure-Activity Relationship

Substances

  • Ligands
  • Nitriles
  • Peptides
  • Proteins
  • Cathepsin L