title: Structure-activity relationship studies of chloromethyl ketone derivatives for selective human chymase inhibitors.
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.
authors.affiliation: Department of Medicinal Chemistry, Kyoto Pharmaceutical University, Japan.
authors.forename: Y
authors.initials: Y
authors.lastname: Hayashi
authors.forename: K
authors.initials: K
authors.lastname: Iijima
authors.forename: J
authors.initials: J
authors.lastname: Katada
authors.forename: Y
authors.initials: Y
authors.lastname: Kiso
mesh_terms: 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
chemical_list: D007659:Ketones; D015842:Serine Proteinase Inhibitors; D012697:Serine Endopeptidases; D053818:Chymases