新型异恶唑啉二酰肼类化合物的设计、合成与杀虫活性研究——作为 GABA 受体抑制剂。
Design, Synthesis, and Insecticidal Activity of Novel Isoxazoline Diacylhydrazine Compounds as GABA Receptor Inhibitors.
机构信息
National Key Laboratory of Green Pesticide, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Huaxi District, Guiyang 550025, China.
Key Laboratory of Agri-Food Safety of Anhui Province, School of Resources and Environment, Anhui Agricultural University, Hefei 230036, China.
出版信息
J Agric Food Chem. 2023 May 3;71(17):6561-6569. doi: 10.1021/acs.jafc.2c08880. Epub 2023 Apr 19.
A series of isoxazoline derivatives containing diacylhydrazine moieties were designed and synthesized as potential insecticides. Most of these derivatives exhibited good insecticidal activities against , and some compounds exhibited excellent insecticidal activities against . Especially, showed outstanding insecticidal activity against (LC = 0.37 μg/mL), which was superior to that of ethiprole (LC = 2.84 μg/mL) and tebufenozide (LC = 15.3 μg/mL) and similar to that of fluxametamide (LC = 0.30 μg/mL). Remarkably, the insecticidal activity of against (LC = 1.72 μg/mL) was superior to that of chlorantraniliprole (LC = 3.64 μg/mL) and tebufenozide (LC = 60.5 μg/mL) but lower than that of fluxametamide (LC = 0.14 μg/mL). The results of electrophysiological experiments, molecular docking, and proteomics experiments indicate that compound acts by interfering with the γ-aminobutyric acid receptor to control pests.
一系列含有二酰肼部分的异恶唑啉衍生物被设计和合成，作为潜在的杀虫剂。这些衍生物大多数对表现出良好的杀虫活性，一些化合物对表现出优异的杀虫活性。特别是对（LC=0.37μg/mL）表现出突出的杀虫活性，优于乙虫腈（LC=2.84μg/mL）和虫酰肼（LC=15.3μg/mL），与氟虫酰胺（LC=0.30μg/mL）相当。值得注意的是，对（LC=1.72μg/mL）的杀虫活性优于氯虫苯甲酰胺（LC=3.64μg/mL）和虫酰肼（LC=60.5μg/mL），但低于氟虫酰胺（LC=0.14μg/mL）。电生理实验、分子对接和蛋白质组学实验的结果表明，化合物通过干扰γ-氨基丁酸受体来控制害虫。
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