Synthesis of 2-(4-substituted-1-piperazinyl) benzimidazoles as H1-antihistaminic agents

R Iemura, T Kawashima, T Fukuda, K Ito…

Index: Iemura; Kawashima; Fukuda; Ito; Tsukamoto Journal of Medicinal Chemistry, 1986 , vol. 29, # 7 p. 1178 - 1183

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Citation Number: 73

Abstract

A series of 2-(4substituted-l-(homo) piperazinyi) benzimidazoles was prepared and tested for Hl-antihistaminic activity in vitro and in vivo. Most of the compounds showed antihistaminic activity and some of the 1-[2-(substituted-oxy) ethyl] derivatives exhibited potent activity. In a structure-activity comparison it was found that the oxygen atom in the 2- (substituted-oxy) ethyl group at the 1-position of the benzimidazole nucleus played an ...