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

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

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(40μg/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(500mg/L)对纹枯病菌的抑制率为50%.

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. Com- pounds 3g and 3h showed fungicidal activity against R. solani with 50% inhibition rate at 500 mg/L.