Multisubstrate inhibitors of dopamine. beta.-hydroxylase. 1. Some 1-phenyl and 1-phenyl-bridged derivatives of imidazole-2-thione

…, WE DeWolf Jr, JS Frazee, E Garvey…

文献索引：Kruse; Kaiser; DeWolf Jr.; Frazee; Garvey; Hilbert; Faulkner; Flaim; Sawyer; Berkowitz Journal of Medicinal Chemistry, 1986 , vol. 29, # 12 p. 2465 - 2472

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被引用次数: 37

摘要

The synthesis and characterization of some l-(phenylalkyl) imidazole-2-thiones as a novel class of “multisubstrate” inhibitors of dopamine@-hydroxylase (DBH) are described. These inhibitors incorporate structural features that resemble both tyramine and oxygen substrates, and as evidenced by steady-state kinetics, they appear to bind both the phenethylamine binding site and the active site copper atom (s) in DBH. A series of structural congeners ...