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首页> 外文会议>International workshop on crop protection chemistry and regulatory harmonization >Synthesis and Herbicidal Activity and Binding Model and 3D-QSAR of 2-Cyano-3-heterocyclemethylaminoacrylates as PSII Electron Transport Inhibitor
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Synthesis and Herbicidal Activity and Binding Model and 3D-QSAR of 2-Cyano-3-heterocyclemethylaminoacrylates as PSII Electron Transport Inhibitor

机译：作为PSII电子传输抑制剂的2-氰基-3-杂丁基氨基丙烯酸酯的合成和除草活性和结合模型及3D QSAR

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@@ 2-Cyanoacrylates are inhibitors of photosystem Ⅱ (PSⅡ) electron transport, which inhibits the growth of weeds by disrupting photosynthetic electron transport at the PSⅡ reaction center. Therefore this kind of compounds can be used as potential herbicide. We have designed and synthesized series of 2cyanoacrylates containing a heterocycle such as pyridine, thiazole, furan, pyrimidine, oxazole, oxadiazole and quinoline groups. Some of them exhibited excellent herbicidal activities. Especially, NK-9717 showed excellent herbicidal activities even at a dose of 75 g/ha. Moreover, it is very safe to corn, which is a major crop in China. We have finished biological test, toxicity test, formulation research, complete analysis research, mechanism research and application evaluation of NK9717 as a novel safe corn herbicide. We found that the N atom on pyridine ring formed a H-bond with the main chain nitrogen atom in Phe265 on the active site, which could explain its high activity.
机译：@@ 2-氰基丙烯酸酯是照相Ⅱ（PSⅡ）电子传输的抑制剂，其通过破坏PSⅡ反应中心的光合电子传输来抑制杂草的生长。因此，这种化合物可用作潜在的除草剂。我们设计了含有嘧啶，噻唑，呋喃，嘧啶，恶毒，恶毒唑和喹啉基团的杂环如杂环的2种丙烯酸酯的设计和合成的杂环系列。其中一些人表现出优异的除草活动。特别是，即使在75克/小时的剂量下，NK-9717也显示出优异的除草活性。此外，对玉米非常安全，这是中国的主要作物。我们已经完成了生物学测试，毒性测试，制定研究，完整的分析研究，机制研究和NK9717的机制研究和应用评估作为新型安全玉米除草剂。我们发现吡啶环上的N原子与活性位点上的PHE265中的主链氮原子形成H键，这可以解释其高活性。

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