Multisubstrate inhibitors of dopamine. beta.-hydroxylase. 2. Structure-activity relationships at the phenethylamine binding site

…, J Wawro, M Wise, KE Flaim, JL Sawyer

Index: Kruse; Kaiser; DeWolf Jr.; Frazee; Ross; Wawro; Wise; Flaim; Sawyer; Erickson Journal of Medicinal Chemistry, 1987 , vol. 30, # 3 p. 486 - 494

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Citation Number: 43

Abstract

1-Aralkylimidazole-2-thiones have been shown to be potent multisubstrate inhibitors of dopamine@-hydroxylase (DBH; EC 1.14. 17.1). In the present study, a series of 1- benzylimidazole-2-thiones was prepared to explore the effects of substitution in the benzyl ring on the inhibition of DBH. A detailed structure-activity relationship for in vitro activity was discovered and this was shown by a modified Hansch analysis to correlate (r= 0.91) with ...