2-氰基-3-甲硫基-3-(4-甲基或6-甲基苯并[d]噻唑-2-氨基)丙烯酸酯类化合物的合成和抗病毒活性研究

Synthesis and Antiviral Activity of(E)-3-(4-or 6-Methylbenzo[d]thiazol-2-yl-amino)-2-cyano-3-(methylthio)acrylate Derivatives

以氰基乙酸和氰基乙酸乙酯为起始原料,采用活性基团拼接的方法,将苯并噻唑基团引入氰基丙烯酸酯中,设计合成了14个含有苯并噻唑基团的氰基丙烯酸酯(酰胺)类化合物3.所有化合物结构经过1H NMR,13C NMR,红外光谱和元素分析确证,并对所合成的目标化合物3进行了室内抗烟草花叶病毒(TMV)和抗黄瓜花叶病毒(CMV)活性测试.结果表明该类化合物具有一定的抗TMV和抗CMV活性.在0.5 mg/mL时,化合物3b,3c,3d对CMV表现出较好的活体治疗活性,抑制率分别为46.3%,45.1%,43.7%.

Starting from ethyl cyanoacetate（cyanoacetic acid）,fourteen title compounds were designed and synthesized by introducing the biologically active benzothiazolyl into the structure of cyanoacrylate.The structures of the new compounds synthesized were confirmed by 1H NMR,13C NMR,IR spectra and elemental analysis.The result of bioassay showed that some target compounds have moderate anti-TMV or anti-CMV activity.The compounds 3b,3c and 3d had good antiviral activity against TMV and CMV with the inhibitory rate of 46.3%,45.1% and 43.7% at the concentration of 0.5 mg/mL.