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有机化学
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有机化学 ›› 2010, Vol. 30 ›› Issue (04): 558-563. 上一篇    下一篇

研究论文

4-(N-乙酰氨基)-3-(4-芳基噻唑-2-氨基)苯甲酸乙酯的合成与生物活性

夏林，胡艾希*，彭俊梅   

  1. (湖南大学化学化工学院 长沙 410082)
  • 收稿日期:2009-08-06 修回日期:2009-11-15 发布日期:2010-04-28
  • 通讯作者: 胡艾希 E-mail:axhu@hnu.cn
  • 基金资助:

    国家科技支撑计划2006BAE01A01－4资助.

Synthesis and Biological Activity of Ethyl 4-Acetamido- 3-(4-arylthiazol-2-yl-amino)benzoate

Xia Lin Hu Aixi* Peng Junmei   

  1. College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082)
  • Received:2009-08-06 Revised:2009-11-15 Published:2010-04-28

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以3-氨基-4-乙酰氨基苯甲酸乙酯为原料设计合成了18种4-(N-乙酰氨基)-3-(4-芳基噻唑-2-基)-苯甲酸乙酯新化合物. 化合物结构经质谱, 元素分析, 1H NMR和13C NMR确证. 生物活性实验结果表明, 化合物3d, 3h, 3p (40 μg/mL)对神经氨酸酶(NA)的抑制率分别为36.02%, 33.40%, 42.05%; 化合物3g, 3h (500 mg/L)对纹枯病菌的抑制率为50%.

关键词: 4-(N-乙酰氨基)-3-(4-芳基噻唑-2-氨基)苯甲酸乙酯, 神经氨酸酶, 合成, 生物活性

A series of ethyl 4-acetamido-3-(4-arylthiazol-2-yl-amino)benzoates were synthesized and evaluated for their ability to inhibit neuraminidase (NA). Their structures were clearly established by MS, elemental analysis, 1H NMR and 13C NMR techniques. The inhibition rates of three compounds 3d, 3h and 3p against influenza A neuraminidase were 36.02%, 33.40% and 42.05% respectively at 40 μg/mL. Compounds 3g and 3h showed fungicidal activity against R. solani with 50% inhibition rate at 500 mg/L.

Key words: ethyl 4-acetamido-3-(4-arylthiazol-2-yl-amino)benzoate, synthesis, neuraminidase, biological activity