Synthesis,biological evaluation and SAR studies of benzimidazole derivatives as H1-antihistamine agents |
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| Authors: | Xiao Jian Wanga Mei Yang Xib Ji Hua Fub Fu Rong Zhanga Gui Fang Chenga Da Li Yina Qi Dong Youb a |
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| Institution: | Department of Medicinal Chemistry, Beijing Key Laboratory of Active Substances Discovery and Drugability Evaluation, State Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica,Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100050, China ; School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China |
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| 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 anti-PAF activity and decreased potency on hERG compared to astermizole.Hence compound 17d could serve as anti-allergic agent for further development. |
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| Keywords: | Benzinudazole derivatives Antihistamine activity SAR Anti-PAF activity hERG |
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