发现含有二硫缩醛部分的吡啶并[1,2-]嘧啶酮类杂环化合物作为新型有潜力的杀虫剂。
Discovery of Pyrido[1,2-]pyrimidinone Mesoionic Compounds Incorporating a Dithioacetal Moiety as Novel Potential Insecticidal Agents.
机构信息
State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Huaxi District, Guiyang 550025, China.
出版信息
J Agric Food Chem. 2021 Dec 22;69(50):15136-15144. doi: 10.1021/acs.jafc.1c05823. Epub 2021 Dec 8.
A series of novel mesoionic pyrido[1,2-]pyrimidinone compounds incorporating a dithioacetal skeleton were designed and synthesized for use as insecticidal agents. The biological activity of the title compounds indicated good to excellent insecticidal activities against bean aphids () and white-backed planthoppers (). Compound showed excellent insecticidal activity against bean aphids () with an LC value of 2.80 μg/mL, exceeding the insecticidal activity of trifluoropyrimidine (LC = 4.20 μg/mL). Proteomics and molecular docking results indicated that compound could act on nicotinic acetylcholine receptors. This study provides support for the application of mesoionic pyrido[1,2-]pyrimidinone compounds containing dithioacetal as novel insecticidal agents.
一系列新型含二硫缩醛骨架的介离子吡啶并[1,2-]嘧啶酮化合物被设计并合成，用作杀虫剂。标题化合物的生物活性表明对豆蚜（）和褐飞虱（）具有良好到优异的杀虫活性。化合物对豆蚜（）表现出优异的杀虫活性，LC 值为 2.80 μg/mL，超过三氟嘧啶（LC = 4.20 μg/mL）的杀虫活性。蛋白质组学和分子对接结果表明，化合物可以作用于烟碱型乙酰胆碱受体。本研究为含二硫缩醛的介离子吡啶并[1,2-]嘧啶酮化合物作为新型杀虫剂的应用提供了支持。
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