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一类双哌嗪季铵盐的合成及镇痛活性

孙崎, 岳彩芹, 叶加*, 李长龄, 程铁明, 李润涛**

  

  1. 1.北京大学药学院 化学生物学系, 北京 100083;
    2.北京大学 天然药物及仿生药物国家重点实验室, 北京 100083
  • 收稿日期:2007-12-09 修回日期:2008-01-10 出版日期:2008-03-15 发布日期:2008-03-15
  • 通讯作者: 叶加*, 李润涛**

Synthesis and analgesic activities studies on bispiperazinium (BPZ) salts

Qi Sun, Cai-Qin Yue, Jia Ye*, Chang-Ling Li, Tie-Ming Cheng, Run-Tao Li**   

  1. 1. Department of Chemical Biology, School of Pharmaceutical Science, Peking University, Beijing 100083, China;
    2. The State Key Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing 100083, China
  • Received:2007-12-09 Revised:2008-01-10 Online:2008-03-15 Published:2008-03-15
  • Contact: Jia Ye*, Run-Tao Li**

摘要:

97-9-G4为先导物, 设计并合成一系列双哌嗪季铵盐, 测定其镇痛活性, 研究其构效关系。合成了8个双哌嗪季铵盐5a-h, 测定了它们的体内镇痛活性, 结果表明先导物97-9-G4中的苯乙基结构为必需的活性基团, 苯环上引入吸电子基团有利于提高活性, 苯环和哌嗪氮原子的距离为两个碳原子时镇痛活性最好。所合成的化合物具有一定的镇痛活性, 但弱于先导化合物97-9-G4, 总结出的构效关系对该类化合物的进一步结构修饰具有重要的指导意义。

关键词: 双哌嗪季铵盐, 双哌嗪季铵盐, 双哌嗪季铵盐, 镇痛, 镇痛, 镇痛, 构效关系, 构效关系, 构效关系, 合成, 合成, 合成

Abstract:

Selecting compound 97-9-G4 as lead compound, a series of bispiperazinium salts 5a-h were designed, synthesized and evaluated for their analgesic activities. The results show that phenylethyl group of 97-9-G4 is a crucial pharmacophore; the introduction of electron-withdrawing group on benzene ring is favorable to the activity.

Key words: Bispiperazinium salt, Bispiperazinium salt, Analgesic activity, Analgesic activity, SAR, SAR, Synthesis, Synthesis

中图分类号: 

Supporting: Foundation item: National Natural Science Foundation of China(Grant No. 20372006 and 20772009).
*Corresponding authors. **Tel.: 86-10-82801504; fax: 86-10-82716956;
*Tel.: 86-10-82802653;