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Synthesis and Insecticidal Activities of Novel Pyrazole Amides Containing Hydrazone Substructures

机译:新型含有Hy亚结构的吡唑酰胺的合成和杀虫活性

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@@ Pyrazole and hydrazone derivatives possess good insecticidal activities; their substructural units are widely used in pesticide design. In an effort to discover new molecules with good insecticidal activities, a series of pyrazole amide derivatives containing hydrazone substructures were synthesised and bioassayed. Bioassays demonstrated that some of the title compounds exhibited notable control of Plutella xylostella (Linnaeus), Helicoverpa armigera (Hiibner), Culex pipiens pallens, Laphygma exigua (Hiibner), Spodoptera litura (Fabricius),Nilaparvata lugens (Stal) and Rhopalosiphummaidis (Fitch) at 5, 10, 0.25, 200, 20, 100 and 500 mg/L, respectively. Comparative molecular field analysis (CoMFA) based on the bioactivities for P. xylostella was studied; the values of q2 and r2 for the CoMFA model were 0. 701 and 0. 964 respectively. Some of the title compounds displayed good and broad-spectrum insecticidal activities against different insect species; the CoMFA model revealed that a bulky and negatively charged group at the 4-position of benzene could enhance insecticidal activity. These results could provide useful information for the design of novel insecticide containing substructural units of pyrazole amide and hydrazone.
机译:吡唑和衍生物具有良好的杀虫活性;它们的子结构单元广泛用于农药设计中。为了发现具有良好杀虫活性的新分子,合成了一系列含有亚结构的吡唑酰胺衍生物并进行了生物分析。生物测定法表明,某些标题化合物对小菜蛾(Plutella xylostella)(Linnaeus),棉铃虫(Helicoverpa armigera)(Hiibner),淡色库蚊(Culex pipiens pallens),拉菲藻(Laphygma exigua)(Hiibner),斜纹夜蛾(Spodoptera litura(Fabricius),斜纹夜蛾(Nilaparhum lumais(Stal))和Rhopalos分别为5、10、0.25、200、20、100和500 mg / L。研究了基于小菜蛾的生物活性的比较分子场分析(CoMFA)。对于CoMFA模型,q2和r2的值分别为0. 701和0. 964。一些标题化合物对不同昆虫种类显示出良好的广谱杀虫活性。 CoMFA模型显示,苯的4位庞大且带负电荷的基团可以增强杀虫活性。这些结果可为设计新型含吡唑酰胺和亚结构单元的杀虫剂提供有用的信息。

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