关键词: 2-氰基-3-苯基丙烯酸酯, 2-氨基-4-甲基苯并[d]噻唑, 合成, 抗病毒活性

In order to explore novel cyanoacrylates with highly antiviral activity, twenty new compounds 4 were synthesized by using ethyl cyanoacetate (cyanoacetic acid) as starting material, in four steps reaction including esterification, condensation, chlorination, and reaction with 2-amino-4-methylbenzo[d]thiazole. All synthesized new compounds were confirmed by IR, ¹H NMR, ¹³C NMR spectra and elemental analysis. The preliminary bioassay revealed that title compounds possessed moderate to anti-CMV, anti-TMV activities at 500 μg•mL^－1 in vivo. Among these compounds such as 4b, 4o and 4q had moderate curative effects against cucumber mosaic virus (CMV) with in-hibitory rate of 45.81%, 43.20% and 43.09%, respectively. The preliminary antiviral bioassay results showed that the curative effects of 4d, 4f, 4h and 4l against tobacco mosaic virus (TMV) were 45.68%, 45.19%, 45.86% and 44.32%, respectively, which is almost similar to that obtained from the standard Ningnanmycin (56.31%, 54.63%).

Key words: 2-cyano-3-phenylacrylate, 2-amino-4-methylbenzo[d]thiazole, synthesis, antiviral activity