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
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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、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。
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关键词:
- 3,5-二甲氧基苯丙烯酰胺 /
- 合成 /
- 抗炎活性
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 (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 aspirin(P<0.05). Conclusion :Compound II3 deserves further investigation. -
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