140945-40-0Relevant academic research and scientific papers
Synthesis and structure-activity relationships of a new series of benzimidazoles as H1-antihistaminic agents
Cuberes, Maria Rosa,Contijoch, Montserrat,Calvet, Carme,Alegre, Julia,Quintana, Jordi Ramon,Frigola, Jordi
, p. 1287 - 1292 (1997)
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.
Derivatives of benzimidazole and their use as antihistamines
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, (2008/06/13)
The present invention relates to novel compounds derived from benzimidazole, characterized in that they correspond to the formula I, or their therapeutically acceptable salts, STR1 in which: R1 and R2, equal or different, represent a hydrogen atom, a halogen, a lower alkyl radical, a hydroxy radical, an alkoxy radical, an alkyl carboxylate radical, an aryl or substituted aryl radical, n may have the values 0 or 1, m may have the values 2 to 4, X, Y, Z and W, equal or different, represents a nitrogen atom or a carbon atom bonded to a hydrogen atom, a halogen or another alkyl, aryl, alkoxycarbonyl, carboxy, hydroxyl, sulfonic and alkylsulfonic radical. The present invention relates also to the treatment of various allergic disorders caused by histamine.
