α-取代-E-3,5-二羟基苯丙烯酸的合成及其抗炎活性  

Synthesis and Anti-inflammatory Activity of α-Substituted-E-3,5-dihydroxyphenylpropenic Acids

作　　者：李静[1] 敖桂珍[1] 绪广林[2] 郑丽玲[1] 张璐[1] 

机构地区：[1]苏州大学药学院,江苏苏州215123 [2]南京师范大学生命科学院新药研究中心,江苏南京210009

出　　处：《合成化学》2010年第1期128-130,共3页Chinese Journal of Synthetic Chemistry

摘　　要：以3,5-二甲氧基苯甲醛为原料,经Perkin反应生成α-取代-E-3,5-二甲氧基苯丙烯酸,然后脱去芳甲醚的甲基合成了三个新的α-取代-E-3,5-二羟基苯丙烯酸(4a^4 c),其结构经1H NMR,IR和MS确证。应用二甲苯致小鼠耳肿胀模型评价4的抗炎活性,结果表明它们均有抗炎活性。其中4b与阳性对照药阿司匹林相比,表现出显著性差异(P<0.05)。Throe novel or-substituted-E-3,5-dihydroxyphenylpropenie acids （ 4a -4c） were synthesized from 3,5-dimethoxybenzaldehyde by Perkin reaction and O-demethylation, and their strueturos were characterized by ^1H NMR, IR and MS. The results of their anti-inflammatory activities against xylene-induced mice ear swelling showed that 4 exhibited certain anti-inflammatory activities. 4b was more potent than aspirin （ P 〈 0.05 ）.

关 键 词：丙烯酸 PERKIN反应 合成 抗炎活性 

分 类 号：O625.52[理学—有机化学] R914.5[理学—化学]