To develop novel 2-cyanoacrylate derivatives with potential bioactivity, a number of 2-cyanoacrylate compounds, including substituted pyrazole or 1,2,3-triazole ring, were designed, prepared, and structurally detected by 1H NMR, 13C NMR, and elemental analysis. The biological assessment displayed that some designed compounds had significant herbicidal activities against Brassica juncea, Chenopodium serotinum, Rumex acetosa, Alopecurus aequalis, Polypogon fugax, and Poa annua at a dosage of 1500 g/ha. Furthermore, some derivatives still expressed satisfactory herbicidal activities against Brassica juncea, Chenopodium serotinum, and Rumex acetosa when the dosage was lowered to 150 g/ha, especially the inhibitory effects of compounds 9a, 9d, 9f, 9i, 10a, 10b, 10e, and 10n against Brassica juncea were all over 80%, compounds 9d, 9f, 9g, 9h, 9i, 10h, 10i, 10m, 10n, and 10o possessed more than 70% inhibition rates against Chenopodium serotinum, and compound 9d indicated 70% herbicidal activity against Rumex acetosa. These results provided an important basis for further design and discovery of biologically active 2-cyanoacrylate compounds.

测试数据显示, 大多数化合物在 500 μg/mL 浓度下对粘虫呈现出 100%的杀死率. 其中 3 个化合物在 100 μg/mL 浓度下 对粘虫的杀死率达 80%～100%, 在浓度降至 20 μg/mL 时, 3 个化合物对粘虫仍表现出 40%～50%的杀虫活性. 3 个化合 物在 500 μg/mL 浓度下对蚜虫显示出 100%的杀虫效果, 在 100 μg/mL 浓度下对蚜虫仍有 70%～100%的杀虫活性. 另外, 2 个化合物在 500 μg/mL 时对朱砂叶螨的防效为 90%～100%.