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