| 苯乙烯基喹啉磺酰胺衍生物的设计、合成与 HIV整合酶抑制活性的研究 |
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| 引用本文： | 曾程初,牛丽亭,平大为,钟儒刚.苯乙烯基喹啉磺酰胺衍生物的设计、合成与 HIV整合酶抑制活性的研究[J].有机化学,2009,29(7):1105-1114. |
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| 作者姓名： | 曾程初 牛丽亭 平大为 钟儒刚 |
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| 作者单位： | 北京工业大学生命科学与生物工程学院,北京,100124 |
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| 基金项目： | 国家自然科学基金，北京市科技新星计划，北京市自然科学基金 |
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| 摘 要： | 在运用比较分子场分析方法(CoMFA)分析了38个苯乙烯基喹啉类衍生物的三维定量构效关系的基础上, 根据立体, 静电以及氢键特征, 设计合成了一系列苯乙烯基喹啉磺酰胺衍生物并考察了它们的HIV整合酶抑制活性, 同时分析了所合成化合物的波谱特点.
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| 关 键 词： | HIV整合酶抑制剂 苯乙烯基喹啉磺酰胺衍生物 Perkin反应 |
| 收稿时间： | 2008-9-18 |
| 修稿时间： | 2008-12-6 |
Design and Synthesis of 2-Styrylquinoline-7-sulfonamide Derivatives as Potential HIV Integrase Inhibitors |
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| Zeng, Chengchu,Niu, Liting,Ping, Dawei,Zhong, Rugang.Design and Synthesis of 2-Styrylquinoline-7-sulfonamide Derivatives as Potential HIV Integrase Inhibitors[J].Chinese Journal of Organic Chemistry,2009,29(7):1105-1114. |
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| Authors: | Zeng Chengchu Niu Liting Ping Dawei Zhong Rugang |
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| Institution: | (College of Life Science & Bioengineering, Beijing University of Technology, Beijing 100124) |
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| Abstract: | According to the steric, electrostatic and H-bonding features of the CoMFA model which was stemmed from the investigation of 38 2-styrylquinoline derivatives, a series of 2-styrylquinoline-7-sulfonamide derivatives were synthesized and evaluated as potential HIV integrase inhibitors. The structures of all compounds were characterized by NMR, IR, ESI-MS and HRMS techniques. |
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| Keywords: | HIV integrase inhibitor 2-styrylquinoline-7-sulfonamide Perkin reaction |
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