Two lead compounds with benzenesulfonamide were found through virtual screening based on the 3D structure of the subunit H of V-ATPase in previous study. 74 benzenesulfonyl derivatives were synthesized and their insecticidal activities were evaluated. The derivatives with propargyl substituents exhibit excellent insecticidal activities against Mythimna separata Walker. The LD₅₀ values of compounds A5.7 (28.0 μg·g⁻¹) and B5.7 (36.4 μg·g⁻¹) were significantly less than that of Celangulin V (344.0 μg·g⁻¹). Furthermore, Isothermal Titration Calorimetry (ITC) data indicate there is a strong binding affinity between A5.7 and V-ATPase Subunit H. These results demonstrate that it is a practical way to develop pesticides targeting at H subunit of V-ATPase.

在先前的研究中，基于V-ATPase H亚基H的3D结构，通过虚拟筛选发现了两种含苯磺酰胺的先导化合物。合成了74个苯磺酰基衍生物，并对其杀虫活性进行了评价。具有炔丙基取代基的衍生物对Mythimna separata Walker表现出优异的杀虫活性。的LD _50个的化合物的值A5.7（28.0微克·克^-1）和B5.7（36.4微克·克^-1）均高于苦皮藤素Ⅴ的显著以下（344.0微克·克^-1）。此外，等温滴定热量法（ITC）数据表明A5.7之间存在很强的结合亲和力 这些结果表明，这是开发针对V-ATPase H亚基的农药的实用方法。