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

作　　者：张美慧[1] 周乐[1] 徐莉英[1] 董金华[1] 计志忠[1] 

机构地区：[1]沈阳药科大学制药工程学院,辽宁沈阳110016

出　　处：《中国药物化学杂志》2004年第6期340-343,共4页Chinese Journal of Medicinal Chemistry

基　　金：辽宁省自然科学基金项目 (No .2 0 0 32 0 4 4 )

摘　　要：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.

关 键 词：药物化学 制备 化学合成 2-(E)-(4-甲磺酰氨基)亚苄基环戊酮 MANNICH碱 抗炎活性 

分 类 号：R914[医药卫生—药物化学]