Structural Diversity Design, Synthesis, and Insecticidal Activity Analysis of Ester-Containing Isoxazoline Derivatives Acting on the GABA Receptor.

To explore insecticides targeting the γ-aminobutyric acid (GABA) receptor, two series of novel isoxazoline derivatives containing sulfonic and carboxylic esters were designed and synthesized. Their insecticidal activities against , , and larvae and their structure-activity relationship were investigated. The sulfonate-containing isoxazoline derivatives () exhibited promising insecticidal activities against the three insect larvae. Compound displayed excellent activities with LC values of 8.32, 5.23, and 0.35 μg/mL at 48 h against , , and larvae, respectively, which were better than or similar to those of avermectin. Furthermore, compound exhibited a faster insecticidal effect than avermectin against . The mode of action of was preliminarily verified by molecular docking, theoretical calculations, and measurement of glutamate decarboxylase and glutamic pyruvic transaminase activities. Compound is a novel insecticidal candidate acting on GABA receptors, which could guide the discovery of isoxazoline insecticides.