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

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

文献索引：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

全文：HTML全文

被引用次数: 4

摘要

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 ...