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阿魏酸及其类似物的合成及其清除自由基活性研究

Investigation of ferulaic acid and its analogs: synthesis and scavenging free radicals

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【作者】 黄华永沈海星郑锦鸿

【Author】 HUANG Hua-yong;SHEN Hai-xing;ZHENG Jin-hong (Department of Chemistry, The Medical College, Shantou University, Shantou 515041 , China; Teaching and Research Group, Shantou Health School, Shantou 515073, China)

【机构】 汕头大学医学院化学教研室汕头市卫生学校理科教研组汕头大学医学院化学教研室 汕头 515041汕头 515073汕头 515041

【摘要】 目的:合成阿魏酸及其类似物并研究其清除1,1-二苯基苦基苯肼自由基(DPPH·)的能力。方法:不同对羟基苯甲醛衍生物和丙二酸进行Knoevenagel缩合反应,得到阿魏酸及其类似物;用体外清除DPPH·测定法检测其清除自由基的能力。结果:合成了9个化合物,其中7个为新报道化合物;在体外清除DPPH·测定中,这些化合物对DPPH·的清除率有较大差异。结论:阿魏酸及其类似物苯环上3,5位取代基可以明显地影响此类化合物清除DPPH·的能力。甲氧基和乙氧基可明显提高活性,溴次之,硝基则降低活性。

【Abstract】 Objective: To synthesize ferulaic acid and its analogs, and exploit the ability of these compounds to scavenge free radicals. Methods: Ferulaic acid and its analogs were synthesized via a Kno-evenagel condensation of different substituted 4-hydroxybenzaldehyde with maloic acid. The ability of the target compound to scavenge free radicals was measured using DPPH·. system. Results: Of nine compounds newly synthesized, seven were firstly reported. Theses compounds showed different scavenging levels on DPPH·. Conclusion: 3, 5-substituted groups on benzene ring of ferulaic acid and its analogs significantly affected the scavenging levels on DPPH·. The scavenging levels were increased by methox- yl, ethoxyl or bromine substituents, but reduced by nitryl substituent on benzene ring.

  • 【文献出处】 中国新药杂志 ,Chinese Journal of New Drugs , 编辑部邮箱 ,2006年06期
  • 【分类号】R284
  • 【被引频次】62
  • 【下载频次】834
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