Synthesis and structure-activity of 4 (5)-(2, 2-diphenylethyl) imidazoles as new α 2-adrenoreceptor antagonists

…, D Giraud-Mangin, C Van der Maesen…

Index: Cordi; Snyers; Giraud-Mangin; Van der Maesen; Van Hoeck; Beuze; Ellens; Napora; Gillet; Gorissen; Calderon; Remacle; Janssens de Varebeke; Van Dorsser; Roba European Journal of Medicinal Chemistry, 1990 , vol. 25, # 7 p. 557 - 568

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Citation Number: 13

Abstract

Abstract 4 (5)-(2, 2-diphenylethyl) imidazole 6a is described as being a potent (pK i= 8.16 for displacement of [3 H] p-amino-clonidine) and selective (selectivity=-log (pK i α 2-pK i α 1)= 81) α 2-adrenoreceptor antagonist (pA 2= 8.73 versus clonidine in the electrically stimulated guinea pig ileum) with additional activity as a norepinephrine uptake inhibitor (IC 50= 0.3 μM). An investigation of the structure-activity relationships of compounds closely related to ...