New chemotypes for cathepsin K inhibitors

Bioorg Med Chem Lett. 2008 Apr 15;18(8):2599-603. doi: 10.1016/j.bmcl.2008.03.036. Epub 2008 Mar 16.

Abstract

Cyano pyrimidine acetylene and cyano pyrimidine t-amine, which belong to a new chemical class, were prepared and tested for inhibitory activities against cathepsin K and the highly homologous cathepsins L and S. The use of novel chemotypes in the development of cathepsin K inhibitors has been demonstrated by derivatives of compounds 1 and 8.

MeSH terms

  • Binding Sites
  • Cathepsin K
  • Cathepsin L
  • Cathepsins / antagonists & inhibitors*
  • Cathepsins / chemistry
  • Cathepsins / metabolism*
  • Cysteine Endopeptidases / metabolism
  • Drug Design
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • Humans
  • Models, Molecular
  • Molecular Structure
  • Structure-Activity Relationship

Substances

  • Enzyme Inhibitors
  • Cathepsins
  • Cysteine Endopeptidases
  • CTSL protein, human
  • Cathepsin L
  • cathepsin S
  • CTSK protein, human
  • Cathepsin K