【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。更多还原

【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.更多还原