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有机化学
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有机化学 ›› 2009, Vol. 29 ›› Issue (07): 1105-1114. 上一篇    下一篇

研究论文

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

曾程初* ; 牛丽亭; 平大为; 钟儒刚   

  1. (北京工业大学生命科学与生物工程学院 北京 100124)
  • 收稿日期:2008-09-18 修回日期:2008-12-06 发布日期:2009-07-22
  • 通讯作者: 曾程初

Design and Synthesis of 2-Styrylquinoline-7-sulfonamide Derivatives as Potential HIV Integrase Inhibitors

Zeng, Chengchu* ; Niu, Liting; Ping, Dawei; Zhong, Rugang   

  1. (College of Life Science & Bioengineering, Beijing University of Technology, Beijing 100124)
  • Received:2008-09-18 Revised:2008-12-06 Published:2009-07-22
  • Contact: Zeng, Chengchu

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被引次数

6 | 1

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.

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

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.

Key words: 2-styrylquinoline-7-sulfonamide, Perkin reaction, HIV integrase inhibitor