引用本文:
郑丽玲, 绪广林, 敖桂珍, 吴周. α-取代的3,5-二甲氧基苯丙烯酸的合成及其抗炎活性[J]. 应用化学,
2008, 25(4): 481-484.
Citation: ZHENG Li-Ling, XU Guang-Lin, AO Gui-Zhen, WU Zhou. Synthesis and Anti-inflammatory Activity of α-Substituted 3,5-Dimethoxyphenylpropenoic Acid Derivatives[J]. Chinese Journal of Applied Chemistry, 2008, 25(4): 481-484.
Citation: ZHENG Li-Ling, XU Guang-Lin, AO Gui-Zhen, WU Zhou. Synthesis and Anti-inflammatory Activity of α-Substituted 3,5-Dimethoxyphenylpropenoic Acid Derivatives[J]. Chinese Journal of Applied Chemistry, 2008, 25(4): 481-484.
α-取代的3,5-二甲氧基苯丙烯酸的合成及其抗炎活性
摘要:
以3,5-二甲氧基苯甲醛为原料,与芳基乙酸经Perkin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。
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关键词:
- α-芳基取代二甲氧基苯丙烯酸
- / Pekin反应
- / 抗炎作用
English
Synthesis and Anti-inflammatory Activity of α-Substituted 3,5-Dimethoxyphenylpropenoic Acid Derivatives
Abstract:
Nine α-substituted 3,5-methoxyphenylpropenoic acids (Ⅰ1~9) were synthesized from 3,5-dimethoxy-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-inflammatory activity,especially compounds Ⅰ6,Ⅰ9 and Ⅰ11,compared with positive control aspirin (P<0.05,P<0.01).
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