Structure-activity relationship studies of chloromethyl ketone derivatives for selective human chymase inhibitors

Bioorg Med Chem Lett. 2000 Feb 7;10(3):199-201. doi: 10.1016/s0960-894x(99)00659-9.

Abstract

Based on the SAR study of a classical chloromethyl ketone derivative, Z-PheCH2Cl 1, a series of compounds were synthesized. Among all the derivatives, compound 21 was found to be a potent human chymase inhibitor with no inhibitory activity against human leukocyte cathepsin G.

MeSH terms

  • Chymases
  • Humans
  • Ketones / chemistry
  • Ketones / pharmacology*
  • Magnetic Resonance Spectroscopy
  • Serine Endopeptidases / drug effects*
  • Serine Proteinase Inhibitors / chemistry
  • Serine Proteinase Inhibitors / pharmacology*
  • Spectrometry, Mass, Fast Atom Bombardment
  • Structure-Activity Relationship

Substances

  • Ketones
  • Serine Proteinase Inhibitors
  • Serine Endopeptidases
  • Chymases