以氰乙酸乙酯(氰乙酸)为起始原料,经酯化、缩合、氯化,然后与2-氨基-4-甲基苯并[d]噻唑反应,合成了20个新化合物4.所有化合物结构经过IR,1H NMR,13C NMR和元素分析确证.初步生物活性测试表明:在500μg·mL-1浓度下,该类化合物4具有一定的抗黄瓜花叶病毒(CMV)及抗烟草花叶病毒(TMV)室内活体治疗活性,其中化合物4b,4o,4q对CMV具有较好的活体治疗活性(抑制率分别为45.81%,43.20%,43.09%),化合物4d,4f,4h,4l对TMV具有较好的活体治疗活性(抑制率分别为45.68%,45.19%,45.86%,44.32%),对照药宁南霉素的活体治疗活性分别为56.31%,54.63%.
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 activi- ties at 500 ktg'mL-~ in vivo. Among these compounds such as 4b, 40 and 4q had moderate curative effects against cucumber mosaic virus (CMV) with inhibitory 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 41 against to- bacco 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%).