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Discovery of Pyrido[1,2-a]pyrimidinone Mesoionic Compounds Incorporating a Dithioacetal Moiety as Novel Potential Insecticidal Agents
Journal of Agricultural and Food Chemistry ( IF 5.7 ) Pub Date : 2021-12-08 , DOI: 10.1021/acs.jafc.1c05823 Jian Zhang 1 , Runjiang Song 1 , Shang Wu 1 , Di Cai 1 , Zengxue Wu 1 , Zhengjun Liu 1 , Deyu Hu 1 , Baoan Song 1
Journal of Agricultural and Food Chemistry ( IF 5.7 ) Pub Date : 2021-12-08 , DOI: 10.1021/acs.jafc.1c05823 Jian Zhang 1 , Runjiang Song 1 , Shang Wu 1 , Di Cai 1 , Zengxue Wu 1 , Zhengjun Liu 1 , Deyu Hu 1 , Baoan Song 1
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A series of novel mesoionic pyrido[1,2-a]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 (Aphis craccivora) and white-backed planthoppers (Sogatella furcifera). Compound 34 showed excellent insecticidal activity against bean aphids (A. craccivora) with an LC50 value of 2.80 μg/mL, exceeding the insecticidal activity of trifluoropyrimidine (LC50 = 4.20 μg/mL). Proteomics and molecular docking results indicated that compound 34 could act on nicotinic acetylcholine receptors. This study provides support for the application of mesoionic pyrido[1,2-a]pyrimidinone compounds containing dithioacetal as novel insecticidal agents.
中文翻译：
发现含有二硫缩醛部分的吡啶并 [1,2-a] 嘧啶酮中离子化合物作为新型潜在杀虫剂
设计并合成了一系列具有二硫缩醛骨架的新型介离子吡啶并[1,2- a ]嘧啶酮化合物，用作杀虫剂。标题化合物的生物活性表明对豆蚜（Aphis craccivora）和白背飞虱（Sogatella furcifera）具有良好至极好的杀虫活性。化合物34对豆蚜（A. craccivora）表现出优异的杀虫活性，LC 50值为2.80 μg/mL，超过了三氟嘧啶的杀虫活性（LC 50 = 4.20 μg/mL）。蛋白质组学和分子对接结果表明化合物34可作用于烟碱型乙酰胆碱受体。本研究为含有二硫缩醛的中离子吡啶并[1,2- a ]嘧啶酮化合物作为新型杀虫剂的应用提供了支持。
更新日期：2021-12-22
中文翻译：
发现含有二硫缩醛部分的吡啶并 [1,2-a] 嘧啶酮中离子化合物作为新型潜在杀虫剂
设计并合成了一系列具有二硫缩醛骨架的新型介离子吡啶并[1,2- a ]嘧啶酮化合物，用作杀虫剂。标题化合物的生物活性表明对豆蚜（Aphis craccivora）和白背飞虱（Sogatella furcifera）具有良好至极好的杀虫活性。化合物34对豆蚜（A. craccivora）表现出优异的杀虫活性，LC 50值为2.80 μg/mL，超过了三氟嘧啶的杀虫活性（LC 50 = 4.20 μg/mL）。蛋白质组学和分子对接结果表明化合物34可作用于烟碱型乙酰胆碱受体。本研究为含有二硫缩醛的中离子吡啶并[1,2- a ]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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