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

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（Ⅱ_1-12），其结构经IR、¹H NMR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。

Abstract: 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 (II_1-12) 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 aspirin(P<0.05). Conclusion ：Compound II₃deserves further investigation.