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有机化学
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有机化学 ›› 2010, Vol. 30 ›› Issue (10): 1559-1562. 上一篇    下一篇

研究简报

双螺环哌嗪季铵盐类化合物的合成及镇痛活性研究

王欣，刘文俊，李刚，叶加，程铁明，李润涛   

  1. (北京大学药学院天然药物及仿生药物国家重点实验室 北京 100191)
  • 收稿日期:2010-05-05 修回日期:2010-05-19 发布日期:2010-05-19
  • 通讯作者: 王欣 E-mail:xinwang@bjmu.edu.cn
  • 基金资助:

    国家自然科学基金

Synthesis and Analgesic Activity of Dispirocyclopiperazinium Ana-logues

WANG Xin, LIU Wen-Jun, LI Gang, YE Jia, CHENG Tie-Ming, LI Run-Tao   

  1. (State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100191)
  • Received:2010-05-05 Revised:2010-05-19 Published:2010-05-19
  • Contact: vivian Wang E-mail:xinwang@bjmu.edu.cn

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1243

被引次数

6 | 1

以己二酰氯、哌嗪类化合物和二溴代物为原料, 合成了一系列未见文献报道的双螺环哌嗪季铵盐类化合物. 通过1H NMR, 13C NMR和元素分析确定了化合物的结构. 在小鼠醋酸扭体模型上初步评价了它们的镇痛活性, 发现多数化合物显示具有较好的镇痛活性, 总结出了相应的构效关系.

关键词: 哌嗪, 螺环哌嗪季铵盐, 合成, 镇痛活性, 构效关系

A series of dispirocyclopiperazinium analogues were synthesized by the reaction of hexanedioyl chloride, piperazine analogues and dibromides. The structures of target compounds were characterized by 1H NMR, 13C NMR spectra and elemental analysis. Preliminary bioassay test indicated that most of the compounds showed significant analgesic activity, and the structure-activity relationship was revealed.

Key words: piperazine, spirocyclopiperazinium, synthesize, analgesic activity, structure-activity relationship