四氢吡咯里嗪并[2,1-c]喹啉衍生物的合成及其镇痛作用考察

Synthesis and analgesic activities of tetrahydropyrrolizino[2,1-c] quinoline derivatives

目的研究5,6,6a,11b-四氢-7H-吡咯里嗪并[2,1-c]喹啉类化合物的镇痛作用构效关系,寻找具有镇痛活性的新型四氢喹啉类化合物。方法以吡里酮为原料,合成系列化合物。用乙酸致小鼠扭体法测定该类化合物的镇痛活性。结果合成了13个目标化合物,经波谱分析确证其结构。镇痛活性试验表明,所合成的部分化合物具有较明显的镇痛作用。结论该类化合物值得进一步研究。

Objective To study the structure-activity relationship（SAR）of the title compounds and search for new potent analgesic agents in tetrahydropyrrolizino[2,1-c] quinoline derivatives.Methods A series of tetrahydropyrrolizino[2,1-c] quinoline derivatives were prepared with a new synthetic schemes.Their analgesic activities were tested by acetic acid-induced mice writhing model.Results Thirteen new compounds were synthesized and their structures were confirmed by the spectral analysis.Some of the target compounds showed remarkably analgesic activities.Conclusions Some target compounds show potent analgesia activities that could be regarded as valuable compounds for further study.