Synthesis, biological evaluation and SAR studies of benzimidazole derivatives as H 1-antihistamine agents

XJ Wang, MY Xi, JH Fu, FR Zhang, GF Cheng…

Index: Wang, Xiao Jian; Xi, Mei Yang; Fu, Ji Hua; Zhang, Fu Rong; Cheng, Gui Fang; Yin, Da Li; You, Qi Dong Chinese Chemical Letters, 2012 , vol. 23, # 6 p. 707 - 710

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Citation Number: 4

Abstract

A series of benzimidazole derivatives have been designed, synthesized and evaluated for H1 antihistamine activity. Six compounds have showed potent antihistamine H1 activity. The primary SAR analysis indicated that benzyl or benzylidinyl substituted on the exo-nitrogen atom and C2 of the benzimidazole were significant. Further experiments indicated that compound 17d displayed excellent activity to reduce mast cell degranulation, moderate ...