Zhang Caixia, Yuan Hanxiao, Hu Yuge, Li Xiuhuan, Gao Yanqing, Ma Zhiqing, Lei Peng
College of Plant Protection, Northwest A&F University, Yangling, Shaanxi 712100, China.
Shaanxi Research Center of Biopesticide Engineering & Technology, Northwest A&F University, Yangling, Xianyang, Shaanxi 712100, China.
J Agric Food Chem. 2023 Feb 9. doi: 10.1021/acs.jafc.2c07910.
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.
为了探索针对γ-氨基丁酸（GABA）受体的杀虫剂，设计并合成了两个系列含磺酸酯和羧酸酯的新型异恶唑啉衍生物。研究了它们对小菜蛾、棉铃虫和粘虫幼虫的杀虫活性及其构效关系。含磺酸盐的异恶唑啉衍生物（）对三种昆虫幼虫表现出有前景的杀虫活性。化合物在48小时时对小菜蛾、棉铃虫和粘虫幼虫的LC值分别为8.32、5.23和0.35μg/mL，表现出优异的活性，优于或与阿维菌素相当。此外，化合物对小菜蛾的杀虫效果比阿维菌素更快。通过分子对接、理论计算以及谷氨酸脱羧酶和谷丙转氨酶活性的测定，初步验证了的作用模式。化合物是一种作用于GABA受体的新型杀虫候选物，可为异恶唑啉类杀虫剂的研发提供指导。
