2-(E)-(4-甲磺酰氨基)亚苄基环戊酮Mannich碱类化合物的合成及抗炎活性

Synthesis and anti-inflammatory activities of Mannich bases of 2-(E)-(4- methanesulfonylamino)benzylidenecyclopentanone

目的设计合成 2 (E) (4 甲磺酰氨基 )亚苄基环戊酮Mannich碱类化合物 ,并对其抗炎活性进行初步评价。方法以环戊酮、4 硝基苯甲醛及胺类化合物为原料 ,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。结果与结论共合成 11个新化合物 ,经IR、1H NMR和MS确证其结构。初步药理实验结果显示 ,化合物 6f、6i具有一定的抗炎活性。

Aim To design and synthesize the Mannich bases of 2 ( E ) (4 methanesulfonylamino)benzylidenecyclopentanone for studying their anti inflammatory activities.Methods The target compounds were synthesized from the cyclopentanone,4 nitrobenzaldehyde and amines,and bioactivities were evaluated with the model of xylene induced ear edema in mice.Results and conclusion Eleven new compounds were obtained and the structures of the compounds were conformed by MS, 1H NMR and IR spectra.Preliminary pharmacological tests showed that two compounds exhibited anti inflammatory activities.