四氢喹啉类化合物的合成及其镇痛活性研究

Synthesis and analgesic activities of 4-(1H-pyrrol-2-yl)-tetrahydroquinoline derivatives

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。

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.