Design and synthesis of 2-alkylbenzimidazole derivatives as novel non-peptide angiotensin Ⅱ AT1 receptor antagonists  

作　　者：Jin Yi Xu Qian Ran Wei Yi Hua Xiao Ming Wu Qiu Juan Wang Jing Zhang 

机构地区：[1]Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China [2]Department of Physiology, China Pharmaceutical University, Nanjing 210009, China

出　　处：《Chinese Chemical Letters》2007年第3期251-254,共4页中国化学快报（英文版）

基　　金：We are thankful to the National Natural Science Foundation of China(No.30371688);Key Fund of Ministry of Education of China(No.03089)for financial support.

摘　　要：A series of 2-alkylbenzimidazole derivatives 9a-n have been designed and synthesized as a novel class of non-peptide angiotensin H AT1 receptor antagonists. The synthesized compounds were evaluated for their antagonism of angiotensin H, induced contraction in the rabbit thoracic aortic ring and the results showed that compounds 9a, 9g and 9j exhibited potent antagonistic activity of AT1 receptor.A series of 2-alkylbenzimidazole derivatives 9a-n have been designed and synthesized as a novel class of non-peptide angiotensin H AT1 receptor antagonists. The synthesized compounds were evaluated for their antagonism of angiotensin H, induced contraction in the rabbit thoracic aortic ring and the results showed that compounds 9a, 9g and 9j exhibited potent antagonistic activity of AT1 receptor.

关 键 词：2-Alkylbenzimidazole AT1 receptor antagonists SYNTHESIS HYPERTENSION 

分 类 号：TQ463.53[化学工程—制药化工] R972.4[医药卫生—药品]