Abstract

In our previous studies, a kind of novel benzenesulfonamides was found to be a candidate insecticidal compounds. It was shown that propargyloxy and sulfonamide groups are pharmacodynamic groups. One hundred and twenty-six (126) naphthalenesulfonamides derivatives with propargyloxy functionality were designed and synthesized, and their insecticidal activities were determined. Some of them showed outstanding activity, with LC₅₀ values as low as 0.202 mg ml⁻¹, much lower than that of the positive control celangulin V (23.9 mg ml⁻¹). In addition, the structure–activity relationships were discussed, and molecular docking was used to verify the binding mode of the compound and the target receptor.

摘要

在我们之前的研究中，发现一种新型苯磺酰胺是一种候选的杀虫化合物。显示炔丙基氧基和磺酰胺基团是药效学基团。设计合成了一百二十六 (126) 种具有炔丙基氧基官能团的萘磺酰胺衍生物，并测定了它们的杀虫活性。其中一些表现出出色的活性，LC ₅₀值低至0.202 mg ml ^-1，远低于阳性对照celangulin V (23.9 mg ml ^-1 )。此外，还讨论了构效关系，并通过分子对接验证了化合物与靶受体的结合方式。