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

Synthesis and the anti-inflammatory activities of Mannich bases of 2-(E)-(4-methanesulfonyl) benzylidene cyclopentanone
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摘要 目的设计合成2-(E)-(4-甲磺酰基)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-甲磺酰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10个新化合物,经1H-NMR和MS确证其结构。初步药理实验结果显示9个目标化合物均具有一定的抗炎活性。 Aim The Mannich bases of 2- ( E )- (4-methanesulfonyl) benzylidene cyclopentanone were designed and synthesized for studying their anti-inflammatory activities. Methods The target compounds were synthesized from cyclopentanone, 4-methanesulfonylbenzaldehyde and amines and their anti-inflammatory activity were evaluated with the model of xylene-induced ear edema in mice. Results and conclusion Ten new compounds are obtained and their structures are identified by MS and ^1H-NMR spectra. Preliminary pharmacological tests show that nine compounds exert anti-inflammatory activities.
出处 《中国药物化学杂志》 CAS CSCD 2005年第4期193-196,i0001,共5页 Chinese Journal of Medicinal Chemistry
基金 辽宁省自然科学基金项目(20032044) 教育部高等学校博士学科点专项科研基金项目(20040163001)
关键词 药物化学 化合物制备 化学合成 2-(E)-(4-甲磺酰基)亚苄基环戊酮 MANNICH碱 抗炎活性 medicinal chemistry compound preparation chemical synthesis 2-( E )-( 4-methanesulfonyl ) benzylidene cyclopentanone Mannich base anti-inflammatory activity
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