α-取代的3，5-二甲氧基苯丙烯酸的合成及其抗炎活性  

Synthesis and Anti-inflammatory Activity of α-Substituted 3,5-Dimethoxyphenylpropenoic Acid Derivatives

作　　者：郑丽玲[1] 绪广林[2] 敖桂珍[1] 吴周[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

出　　处：《应用化学》2008年第4期481-484,共4页Chinese Journal of Applied Chemistry

摘　　要：以3，5-二甲氧基苯甲醛为原料，与芳基乙酸经Perki n反应合成了α-取代3，5-二甲氧基苯丙烯酸化合物（I1～9），化合物I7经铁粉还原得到化合物I10，化合物I10乙酰化生成I11。目标化合物均为新化合物，其结构经过^1H NMR、红外和高分辨质谱测试技术分析确证。二甲苯致小鼠耳肿胀模型的药理初筛结果表明，大部分目标化合物具有抗炎活性，其中，化合物I6、I9和I11与阳性对照Aspirin相比，表现出显著性差异（P〈0．05，P〈0．01），说明其抗炎活性比Aspirin强。Nine α-substituted 3,5-methoxyphenylpropenoic acids （ I1-9 ） were synthesized from 3,5-dime- thoxy-benzaldehyde and aryl acetic acids by Perkin reaction respectively. I10 was obtained through the reduction of I7 with iron power, and I11 was obtained through acetylation of I10. The structures of these novel compounds whose structures were identified by ^1H NMR, IR and HR-MS. Preliminary pharmacological tests on xylene-induced mice ear swelling model demonstrated that most of the target compounds had anti-inflamma- tory activity, especially compounds I6, I9and I11, compared with positive control aspirin （ P 〈 0. 05, P 〈 0.01）.

关 键 词：α-芳基取代二甲氧基苯丙烯酸 Pekin反应 抗炎作用 

分 类 号：O622.5[理学—有机化学]