| Design and synthesis of 2-alkylbenzimidazole derivatives as novel non-peptide angiotensin Ⅱ AT1 receptor antagonists |
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| 作者姓名： | Jin Yi Xu Qian Ran Wei Yi Hua Xiao Ming Wu Qiu Juan Wang Jing Zhang |
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| 作者单位： | Jin Yi Xu a，Qian Ran a，Wei Yi Hua a，Xiao Ming Wu a，*，Qiu Juan Wang b，Jing Zhang ba Department of Medicinal Chemistry，China Pharmaceutical University，Nanjing 210009，Chinab Department of Physiology，China Pharmaceutical University，Nanjing 210009，China |
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| 基金项目： | Acknowledgments 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. |
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| 摘 要： | 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.
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| 关 键 词： | 非肽类血管紧张素ⅡAT1受体拮抗剂 2-烷基苯并咪唑衍生物 设计 合成 高血压 |
| 收稿时间： | 2006-08-31 |
Design and synthesis of 2-alkylbenzimidazole derivatives as novel non-peptide angiotensin II AT1 receptor antagonists |
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| 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. |
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| Authors: | Jin Yi Xu a Qian Ran a Wei Yi Hua a Xiao Ming Wu a Qiu Juan Wang b Jing Zhang ba |
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| Institution: | Jin Yi Xu a,Qian Ran a,Wei Yi Hua a,Xiao Ming Wu a,*,Qiu Juan Wang b,Jing Zhang ba Department of Medicinal Chemistry,China Pharmaceutical University,Nanjing 210009,Chinab Department of Physiology,China Pharmaceutical University,Nanjing 210009,China |
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| Abstract: | 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. |
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| Keywords: | 2-Alkylbenzimidazole AT1 receptor antagonists Synthesis Hypertension |
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