α-芳基-3,5-二甲氧基苯丙烯酰胺的合成及抗炎活性  

Synthesis and anti-inflammatory activity of α-aryl-3,5-dimethoxyphenylpropenamides

作　　者：敖桂珍[1] 郑丽玲[1] 绪广林[2] 李静[1] 

机构地区：[1]苏州大学药学院,苏州215123 [2]南京师范大学生命科学院新药研究中心,南京210097

出　　处：《中国药科大学学报》2009年第4期302-305,共4页Journal of China Pharmaceutical University

摘　　要：目的:寻找高效低毒的非甾体抗炎药。方法:将具有抗炎活性的2-(2,4-二氯苯基)-3-(3,5-二甲氧基苯基)丙烯酸(I)转化为酰胺衍生物,应用二甲苯致小鼠耳肿胀模型评价其抗炎活性。结果:合成了12个新化合物(Ⅱ1-12),其结构经IR、1HNMR和高分辨MS确证。其中化合物Ⅱ3与阴性对照CMC-Na相比呈现显著的抗炎活性(P<0.01),与阳性对照阿司匹林相比有较强的抗炎活性(P<0.05)。结论:化合物Ⅱ3值得进一步研究。Aim:To search for new compounds with stronger anti-inflammatory activities and less gastrointestinal side effects.Methods:2-(2,4-Dichlorophenyl)-3-(3,5-dimethoxyphenyl)-propenoic acid(I) was converted to amides(II).Their anti-inflammatory activities against xylene-induced mice ear swelling were evaluated.Results:Twelve target compounds(II1-12) were synthesized,and their structures were confirmed by IR,1H NMR and HR-MS.II3 exhibited significant anti-inflammatory activity compared with CMC-Na(P<0.01) and aspi...

关 键 词：3 5-二甲氧基苯丙烯酰胺 合成 抗炎活性 

分 类 号：R914[医药卫生—药物化学]