Structure-activity relationship studies of chloromethyl ketone derivatives for selective human chymase inhibitors.
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.
Hayashi
Y
Y
Department of Medicinal Chemistry, Kyoto Pharmaceutical University, Japan.
Iijima
K
K
Katada
J
J
Kiso
Y
Y
D053818:Chymases; D006801:Humans; D007659:Ketones / Q000737:chemistry / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D012697:Serine Endopeptidases / Q000187:drug effects*; D015842:Serine Proteinase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D016339:Spectrometry, Mass, Fast Atom Bombardment; D013329:Structure-Activity Relationship
D007659:Ketones; D015842:Serine Proteinase Inhibitors; D012697:Serine Endopeptidases; D053818:Chymases