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新型 6-吡唑基-2-吡啶甲酸类除草剂的合成、生物活性及作用机制研究。

Investigation into the Synthesis, Bioactivity, and Mechanism of Action of the Novel 6-Pyrazolyl-2-picolinic Acid as a Herbicide.

机构信息

Innovation Center of Pesticide Research, Department of Applied Chemistry, College of Science, China Agricultural University, Beijing 100193, China.

Key Laboratory of National Forestry and Grassland Administration on Pest Chemical Control, China Agricultural University, Beijing 100193, China.

出版信息

J Agric Food Chem. 2024 Apr 17;72(15):8840-8848. doi: 10.1021/acs.jafc.3c08517. Epub 2024 Apr 3.

DOI:10.1021/acs.jafc.3c08517
PMID:38570314
Abstract

A series of new 4-amino-3,5-dicholo-6-(5-aryl-substituted-1-pyrazol-1-yl)-2-picolinic acid compounds were designed and prepared to discover herbicidal molecules. The inhibitory activities of all new compounds against the root growth of were assayed. On the whole, the new synthesized compounds displayed good inhibition effects and had excellent herbicidal activities on root growth of weed at 500 μM. Importantly, a selection of compounds demonstrated comparable herbicidal properties to picloram. At the dosage of 250 g/ha, most of the compounds showed a 100% postemergence herbicidal activity to control and . Using compound V-2, the mechanism of action was investigated based on a phenotype study using AFB5-deficient . It was found that the novel 6-pyrazolyl-2-picolinic acids were auxinic compounds. In addition, it was proposed that V-2 may be an immune activator due to its upregulation of defense genes and the increased content of jasmonic acid.

摘要

一系列新的 4-氨基-3,5-二氯-6-(5-芳基取代-1-吡唑-1-基)-2-吡啶甲酸化合物被设计和制备,以发现除草分子。所有新化合物对杂草根生长的抑制活性都进行了测定。总的来说,新合成的化合物在 500μM 时对杂草根生长表现出良好的抑制作用和优异的除草活性。重要的是,一些化合物表现出与 picloram 相当的除草特性。在 250g/ha 的剂量下,大多数化合物对 和 具有 100%的苗后除草活性。使用化合物 V-2,基于 AFB5 缺陷型 的表型研究,对作用机制进行了研究。结果发现,新型 6-吡唑基-2-吡啶甲酸是植物生长素类化合物。此外,由于其防御基因的上调和茉莉酸含量的增加,V-2 可能是一种免疫激活剂。

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