N-(3，4-二甲氧基苯乙基)-4取代苯酰胺类化合物的合成与镇痛活性研究

Synthesis and analgesic activity evaluation of N-(3,4-dimethoxyphenethyl)-4-subsitituted benzamids

目的:合成N-(3,4-二甲氧基苯乙基)-4取代苯酰胺类化合物,寻找并合成具有镇痛活性的新型化合物。方法:以经典Nav1.8离子通道抑制剂A-803467的结构为起点,设计合成新型N-(3,4-二甲氧基苯乙基)-4取代苯酰胺类化合物。用小鼠扭体实验和小鼠辣椒素致急性疼痛模型对所合成的目标化合物进行镇痛活性评价。结果:合成了3个化合物,经1H-NMR和MS确证其结构。动物实验表明所合成的3个化合物均表现出明显镇痛活性(P<0.05)。结论:本研究所设计合成的化合物具有作为新型非阿片类镇痛药的开发潜力。

Objective ： To synthesize N- （3,4-dimethoxyphenethyl） -4-subsitituted benzamides and search for new analgesic agents. Methods： Based on the marked analgesic agent, A-803467, the objective substances were designed and synthesized. The analgesic biological activities were evaluated by acetic acid-induced writhing model and eapsaiein-induced pain model in mice. Each group consisted of 10 mice, and their behaviors were recorded and evaluated. Results：Three compounds were synthesized and their structures were confirmed by ^1H-NMR and MS. All the compounds showed analgesic activities. Conclusion：These compounds can be regarded as valuable targets for further study.