2-Phenyl-9H-purine-6-carbonitrile derivatives as selective cathepsin S inhibitors

Bioorg Med Chem Lett. 2010 Aug 1;20(15):4447-50. doi: 10.1016/j.bmcl.2010.06.049. Epub 2010 Jun 15.

Abstract

Starting from previously disclosed equally potent cathepsin K and S inhibitor 4-propyl-6-(3-trifluoromethylphenyl)pyrimidine-2-carbonitrile 1, a novel 2-phenyl-9H-purine-6-carbonitrile scaffold was identified to provide potent and selective cathepsin S inhibitors.

MeSH terms

  • Catalytic Domain
  • Cathepsin K / antagonists & inhibitors
  • Cathepsin K / metabolism
  • Cathepsins / antagonists & inhibitors*
  • Cathepsins / metabolism
  • Cell Line
  • Computer Simulation
  • Humans
  • Nitriles / chemical synthesis
  • Nitriles / chemistry*
  • Nitriles / pharmacology
  • Protease Inhibitors / chemical synthesis
  • Protease Inhibitors / chemistry*
  • Protease Inhibitors / pharmacology
  • Purines / chemical synthesis
  • Purines / chemistry*
  • Purines / pharmacology
  • Pyrimidines / chemistry

Substances

  • 2-phenyl-9H-purine-6-carbonitrile
  • Nitriles
  • Protease Inhibitors
  • Purines
  • Pyrimidines
  • Cathepsins
  • cathepsin S
  • Cathepsin K
  • pyrimidine