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.

中文翻译：

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N-（4-氰基-1-苯基-1 H-吡唑-5-基）-1,3-二苯基-1 H-吡唑-4-羧酰胺衍生物的 设计，合成和杀虫活性†

虫精胺受体是开发新型杀虫剂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-1 H-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）-1 H-吡唑-5-基）-1-（4-氟苯基）-3-苯基-1 H-吡唑-4-羧酰胺（5g）对小菜蛾表现出84％的杀幼虫活性在0.1 mg L ^-1的浓度下。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。