Structure-activity relationships for 2-substituted imidazoles as. alpha. 2-adrenoceptor antagonists

JM Caroon, RD Clark, AF Kluge, R Olah…

Index: Caroon, Joan M.; Clark, Robin D.; Kluge, Arthur F.; Olah, Ronald; Repke, David B.; et al. Journal of Medicinal Chemistry, 1982 , vol. 25, # 6 p. 666 - 670

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Citation Number: 30

Abstract

Several 2 4 (1, 4-benzodioxan-2-yl) alkyl] imidazoles were prepared and evaluated for their blocking activity and relative selectivity on presynaptic (az) and postsynaptic (a1) receptors in the isolated rat vas deferens. 1-Ethyl-2-[(14-benzodioxan-2-yl) methyl] imidazole (13) was the most selective a2-adrenoceptor antagonist of the series and was, for practical purposes, devoid of al-adrenoceptor antagonist activity. The lipophilicity of 13 (log D= 2.31) indicated ...