2-甲基-5-(E)-(邻甲氧基苯亚甲基)环戊酮Mannich碱类化合物的合成及其抗炎活性

Synthesis and antiinflammatory activity of the Mannich bases of 2-methyl-5-(E)-(2-methoxybenzylidene)cyclopentanone

目的设计合成 2 甲基 5 (E) (邻甲氧基苯亚甲基 )环戊酮曼尼希碱类化合物 ,并对其抗炎活性进行初步评价。方法以N 环戊烯基吗啉、邻甲氧基苯甲醛及多种胺类为原料 ,经多步反应合成目标化合物 ,并以二甲苯致小鼠耳肿胀模型测试目标化合物的抗炎活性。结果共合成 8个新化合物 ,经IR ,1H NMR和MS确证其结构。其中两个化合物的抗炎活性与阿司匹林相当。结论羰基α位被烷基取代的环戊酮曼尼希碱仍具有较强的抗炎作用。

Aim To design and synthesize the Mannich bases of 2-methyl-5-(E)-(2-methoxybenzylidene)cyclopentanone,and to study their antiinflammatory activity.Methods The target compounds were synthesized from the cyclopentanone,o-methoxybenzaldehyde and amines and were evaluated with the model of xylene-induced ear edema in mice.Results Eight new compounds were obtained and two of them exerted antiinflammatory activity similar to that of Aspirin.Conclusion Preliminary pharmacological tests showed that two of the Mannich bases of 2-methyl-5-(E)-(2-methoxybenzylidene)cyclopentanone exerted appreciable inhibitory effects on xylene-induced ear edema in mice.