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α-芳基-3,5-二甲氧基苯丙烯酰胺的合成及抗炎活性

敖桂珍, 郑丽玲, 绪广林, 李静

敖桂珍, 郑丽玲, 绪广林, 李静. α-芳基-3,5-二甲氧基苯丙烯酰胺的合成及抗炎活性[J]. 中国药科大学学报, 2009, 40(4): 302-305.
引用本文: 敖桂珍, 郑丽玲, 绪广林, 李静. α-芳基-3,5-二甲氧基苯丙烯酰胺的合成及抗炎活性[J]. 中国药科大学学报, 2009, 40(4): 302-305.
AO Gui-zhen, ZHENG Li-ling, XU Guang-lin, LI Jing. Synthesis and anti-inflammatory activity of α-aryl-3,5-dimethoxyphenylpropenamides[J]. Journal of China Pharmaceutical University, 2009, 40(4): 302-305.
Citation: AO Gui-zhen, ZHENG Li-ling, XU Guang-lin, LI Jing. Synthesis and anti-inflammatory activity of α-aryl-3,5-dimethoxyphenylpropenamides[J]. Journal of China Pharmaceutical University, 2009, 40(4): 302-305.

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(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。
    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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  • 刊出日期:  2009-08-24

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