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烷基砜:靶向囊泡型乙酰胆碱转运体的新型化学骨架引领新一代杀虫剂的诞生。

Alkylsulfones: novel chemical scaffolds targeting the vesicular acetylcholine transporter usher in a new generation of insecticides.

作者信息

Holland Robert A, Crossthwaite Andrew

机构信息

Syngenta, Bioscience, Jealott's Hill International Research Centre, Bracknell, UK.

出版信息

Pest Manag Sci. 2025 May;81(5):2424-2426. doi: 10.1002/ps.8462. Epub 2024 Oct 5.

DOI:10.1002/ps.8462
PMID:39367720
Abstract

Insecticides targeting the nervous system have been the most widely used to control arthropod pests due to their fast onset of action leading to efficient crop protection. With their continued use, resistance has and will become an inevitable challenge that demands continued efforts in identifying and developing new insecticidal chemistries acting on novel targets. In a recent publication, the results of a comprehensive study investigating the mode of action of novel chemical scaffolds based on the 2-(3-ethylsulfonyl-2-pyridyl)-heterocycles, alkylsulfones, was presented, concluding that their primary target is the vesicular acetylcholine transporter. © 2024 Society of Chemical Industry.

摘要

由于作用迅速能有效保护作物,针对神经系统的杀虫剂一直是控制节肢动物害虫最广泛使用的方法。随着它们的持续使用,抗性已经并将成为一个不可避免的挑战,这需要持续努力来识别和开发作用于新靶点的新型杀虫化学物质。在最近的一篇出版物中,展示了一项全面研究的结果,该研究调查了基于2-(3-乙基磺酰基-2-吡啶基)-杂环、烷基砜的新型化学支架的作用模式,得出结论其主要靶点是囊泡乙酰胆碱转运体。© 2024化学工业协会。

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Alkylsulfones: novel chemical scaffolds targeting the vesicular acetylcholine transporter usher in a new generation of insecticides.烷基砜:靶向囊泡型乙酰胆碱转运体的新型化学骨架引领新一代杀虫剂的诞生。
Pest Manag Sci. 2025 May;81(5):2424-2426. doi: 10.1002/ps.8462. Epub 2024 Oct 5.
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A novel insecticide cybenzoxasulfyl potently binds to vesicular acetylcholine transporter and disrupts the storage and release of acetylcholine in insects.
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A novel class of insecticidal alkylsulfones are potent inhibitors of vesicular acetylcholine transport.一类新型的杀虫烷基砜类化合物是囊泡乙酰胆碱转运的强效抑制剂。
Pestic Biochem Physiol. 2024 May;201:105854. doi: 10.1016/j.pestbp.2024.105854. Epub 2024 Mar 12.
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Spiroindolines identify the vesicular acetylcholine transporter as a novel target for insecticide action.螺环吲哚啉类化合物鉴定囊泡型乙酰胆碱转运体为新型杀虫剂作用靶标。
PLoS One. 2012;7(5):e34712. doi: 10.1371/journal.pone.0034712. Epub 2012 May 1.
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IRAC: Mode of action classification and insecticide resistance management.IRAC:作用方式分类与杀虫剂抗性管理。
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The VAChTY49N mutation provides insecticide-resistance but perturbs evoked cholinergic neurotransmission in Drosophila.VAChTY49N 突变提供了抗药性,但扰乱了果蝇中的诱发胆碱能神经递质传递。
PLoS One. 2018 Sep 11;13(9):e0203852. doi: 10.1371/journal.pone.0203852. eCollection 2018.
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Insecticide resistance management and industry: the origins and evolution of the Insecticide Resistance Action Committee (IRAC) and the mode of action classification scheme.杀虫剂耐药性管理与行业:杀虫剂耐药性行动委员会(IRAC)的起源与演变,以及作用模式分类方案。
Pest Manag Sci. 2021 Jun;77(6):2609-2619. doi: 10.1002/ps.6254. Epub 2021 Jan 28.
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Choline acetyltransferase and vesicular acetylcholine transporter are required for metamorphosis, reproduction, and insecticide susceptibility in Tribolium castaneum.胆碱乙酰转移酶和囊泡乙酰胆碱转运体是拟谷盗完成变态、繁殖和对杀虫剂敏感所必需的。
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Regulation of cholinergic activity by the vesicular acetylcholine transporter.囊泡型乙酰胆碱转运体对胆碱能活性的调节。
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Mesoionic insecticides: a novel class of insecticides that modulate nicotinic acetylcholine receptors.中离子型杀虫剂:一类新型的可调节烟碱型乙酰胆碱受体的杀虫剂。
Pest Manag Sci. 2017 Apr;73(4):796-806. doi: 10.1002/ps.4496. Epub 2017 Feb 1.

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