Citation: Jin Yi Xu, Qian Ran, Wei Yi Hua, Xiao Ming Wu, Qiu Juan Wang, Jing Zhang. Design and synthesis of 2-alkylbenzimidazole derivatives as novel non-peptide angiotensin Ⅱ AT₁ receptor antagonists[J]. Chinese Chemical Letters, ;2007, 18(3): 251-254. doi: 10.1016/j.cclet.2006.12.029 shu

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

a Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China;
b Department of Physiology, China Pharmaceutical University, Nanjing 210009, China

Received Date: 31 August 2006

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

A series of 2-alkylbenzimidazole derivatives 9a-n have been designed and synthesized as a novel class of non-peptide angiotensin Ⅱ AT₁ receptor antagonists. The synthesized compounds were evaluated for their antagonism of angiotensin Ⅱ, 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.
- 2-Alkylbenzimidazole,
- AT₁receptor antagonists,
- Synthesis,
- Hypertension
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