Design, synthesis and insecticidal activities of N-(4-cyano-1-phenyl-1H-pyrazol-5-yl)-1,3-diphenyl-1H-pyrazole-4-carboxamide derivatives

Lv Xian-Hai; Xiao Jin-Jing; Ren Zi-Li; Chu Ming-Jie; Wang Peng; Meng Xiang-Feng; Li Dong-Dong; Cao Hai-Qun

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Design, synthesis and insecticidal activities of N-(4-cyano-1-phenyl-1H-pyrazol-5-yl)-1,3-diphenyl-1H-pyrazole-4-carboxamide derivatives

机译：N-（4-氰基-1-苯基-1H-吡唑-5-基）-1,3-二苯基-1H-吡唑-4-羧酰胺衍生物的设计，合成及杀虫活性

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Insect ryanodine receptor is one of the promising targets for the development of novel insecticides. In order to search for potent insecticides targeting the ryanodine receptor (RyR), a series of novel diphenyl-1H-pyrazole derivatives with cyano substituent were designed and synthesized. Their insecticidal activities against diamondback moth (Plutella xylostella) indicated that most of the compounds showed moderate to high activities at the four concentrations. Among these compounds, N-(4-cyano-1-(4-fluorophenyl)-1H-pyrazol-5-yl)-1-(4-fluorophenyl)-3-phenyl-1H-pyrazole-4-carboxamide (5g) showed 84% larvicidal activity against Plutella xylostella at the concentration of 0.1 mg L-1. Molecular docking showed the predicted binding mode between 5g and protein receptor, which could suggest that the title compounds were the possible activators of insect RyR.

机译：虫精胺受体是新型杀虫剂开发的有希望的目标之一。为了寻找针对ryanodine受体（RyR）的有效杀虫剂，设计并合成了一系列具有氰基取代基的新型二苯基-1H-吡唑衍生物。它们对小菜蛾（Plutella xylostella）的杀虫活性表明，大多数化合物在这四个浓度下均表现出中等至高活性。在这些化合物中，N-（4-氰基-1-（4-氟苯基）-1H-吡唑-5-基）-1-（4-氟苯基）-3-苯基-1H-吡唑-4-羧酰胺（5g）在0.1 mg L-1的浓度下对小菜蛾显示84％的杀幼虫活性。分子对接显示了预期的5g与蛋白质受体之间的结合模式，这可能表明标题化合物可能是昆虫RyR的激活剂。

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《RSC Advances》 |2015年第68期|共7页
作者
Lv Xian-Hai; Xiao Jin-Jing; Ren Zi-Li; Chu Ming-Jie; Wang Peng; Meng Xiang-Feng; Li Dong-Dong; Cao Hai-Qun;
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机译：N-（4-氰基-1-苯基-1H-吡唑-5-基）-1,3-二苯基-1H-吡唑-4-羧酰胺衍生物的设计，合成及杀虫活性
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机译：N - （苯乙烯氧基苄基） - 吡唑苄酰胺衍生物的合成和杀虫活性

Design, synthesis and insecticidal activities of N-(4-cyano-1-phenyl-1H-pyrazol-5-yl)-1,3-diphenyl-1H-pyrazole-4-carboxamide derivatives

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