Synthesis and structure-activity relationships of a new series of benzimidazoles as H1-antihistaminic agents

Article abstract of DOI:10.1248/cpb.45.1287

New 2-(4-(4-azolylbutyl)piperazinyl)-, 2-(4-(4- azolylbutyl)piperazinylmethyl)- 2-(4-(4-azolylbutyl)homopiperazinyl)- and 2- (4-(4-azolylbutyl)homopiperazinylmethyl)benzimidazoles were synthesized characterized and tested for in vitro and in vivo H₁-antihistaminic activity. Structure-activity relationships implied that the best anti histaminic activity required the simultaneous presence of a homopiperazinylbenzimidazole system (or a methylene linker between the benzimidazole and the piperazine rings) and an unsubstituted pyrazole ring. 1-(2-Ethoxyethyl)-2-{4-[4-(pyrazol-1-yl)batyl]homopiperazin-1- yl}benzimidazole (17), as its dimaleate salt, has been chosen for further development.

Full text of DOI:10.1248/cpb.45.1287

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