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四氢喹啉类化合物的合成及其镇痛活性研究
引用本文:刘永福,吴丽颖,刘秀洁,王玉玲,宋宏锐.四氢喹啉类化合物的合成及其镇痛活性研究[J].中国药物化学杂志,2007,17(3):144-147.
作者姓名:刘永福  吴丽颖  刘秀洁  王玉玲  宋宏锐
作者单位:沈阳药科大学,制药工程学院,辽宁,沈阳,110016
摘    要:目的寻找具有镇痛活性的新型四氢喹啉类化合物,探讨4-(1H-吡咯-2-基)-1,2,3,4-四氢喹啉类化合物镇痛作用的构效关系。方法以4-(1H-吡咯-2-基)-1,2,3,4-四氢喹啉类化合物为母体,合成系列化合物。用醋酸致小鼠扭体法测定该类化合物的镇痛活性。结果与结论合成了20个新化合物,经1H-NMR和MS确证其结构。镇痛活性试验表明,所合成的部分化合物具有明显的镇痛作用,值得进一步研究。

关 键 词:1  2  3  4-四氢喹啉  镇痛活性  构效关系
文章编号:1005-0108(2007)03-0144-04
收稿时间:2006-11-02
修稿时间:2006-11-02

Synthesis and analgesic activities of 4-(1H-pyrrol-2-yl)-tetrahydroquinoline derivatives
LIU Yong-fu,WU Li-ying,LIU Xiu-jie,WANG Yu-ling,SONG Hong-rui.Synthesis and analgesic activities of 4-(1H-pyrrol-2-yl)-tetrahydroquinoline derivatives[J].Chinese Journal of Medicinal Chemistry,2007,17(3):144-147.
Authors:LIU Yong-fu  WU Li-ying  LIU Xiu-jie  WANG Yu-ling  SONG Hong-rui
Institution:School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China
Abstract:Aim To search for new potent analgesic agents with tetrahydroquinoline structure and to study the structure-activity relationship(SAR) of the title compounds.Methods A series of 4-(1H-pyrrol-2-yl)-tetrahydroquinoline derivatives was prepared with a new synthetic route.Their analgesic activities were tested by acetic acid-induced mice writhing model.Results and conclusion Twenty new compounds were synthesized and their structures were confirmed by 1H-NMR and MS.Some of the target compounds showed remarkable analgesic activities.Some target compounds show potent analgesia activities and could be regarded as valuable compounds for further study.
Keywords:tetrahydroquinoline  analgesic activity  structure-activity relationship
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