5-Aminopyrimidin-2-ylnitriles as Cathepsin K Inhibitors

Bioorg Med Chem Lett. 2009 Mar 15;19(6):1658-61. doi: 10.1016/j.bmcl.2009.01.110. Epub 2009 Feb 6.

Abstract

A series of pyrimidine nitrile inhibitors of Cathepsin K with reduced glutathione reactivity has been identified and Molecular Core Matching (MoCoM) has been used to quantify the effect of an amino substituent at C5.

MeSH terms

  • Cathepsin K
  • Cathepsins / antagonists & inhibitors*
  • Cathepsins / chemistry
  • Chemistry, Pharmaceutical / methods
  • Cysteine Proteinase Inhibitors / chemical synthesis*
  • Cysteine Proteinase Inhibitors / pharmacology
  • Drug Design
  • Humans
  • Lysosomes / enzymology
  • Models, Chemical
  • Molecular Structure
  • Nitriles / chemical synthesis*
  • Osteoarthritis / drug therapy
  • Osteoclasts
  • Osteoporosis / drug therapy
  • Pyrimidines / chemistry
  • Structure-Activity Relationship
  • Technology, Pharmaceutical / methods

Substances

  • Cysteine Proteinase Inhibitors
  • Nitriles
  • Pyrimidines
  • Cathepsins
  • CTSK protein, human
  • Cathepsin K