Synthesis and Bioactivities Evaluation of Novel Anthranilic Diamides Containing N‐(tert‐Butyl)benzohydrazide Moiety as Potent Ryanodine Receptor Activator,Chinese Journal of Chemistry

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Synthesis and Bioactivities Evaluation of Novel Anthranilic Diamides Containing N‐(tert‐Butyl)benzohydrazide Moiety as Potent Ryanodine Receptor Activator
Chinese Journal of Chemistry ( IF 5.5 ) Pub Date : 2019-04-30 , DOI: 10.1002/cjoc.201900073
Yunyun Zhou ₁ , Wei Wei ₂ , Liangliang Zhu ₁ , Yuxin Li ₃

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Anthranilic diamides have been proven to be a class of efficacious and safe insecticides targeting ryanodine receptors (RyRs) during the last decade. In order to develop innovative scaffolds with high insecticidal activity, two series of N‐pyridylpyrazole derivatives containing N‐(tert‐butyl)benzohydrazide substructures were designed and synthesized. Their insecticidal activities against oriental armyworm (Mythimna separata) and diamondback moth (Plutella xylostella) were evaluated. Preliminary bioassay results revealed that some of the new compounds exhibited good insecticidal activity against the oriental armyworm and diamondback moth. The mode of action of these compounds were verified using calcium‐imaging technique and the results showed that some new compounds could effectively modulate the insect cytosolic Ca²⁺ level, and break the cellular calcium homeostasis, indicating some of these compounds were potent activators of the RyRs.

中文翻译：

新型含N-（叔丁基）苯甲酰肼部分为强效Ryanodine受体激活剂的邻氨基苯甲酰胺的合成和生物活性评估

在过去的十年中，邻氨基苯甲酰胺已被证明是针对瑞丹素受体（RyRs）的一类有效且安全的杀虫剂。为了开发具有高杀虫活性的创新支架，设计并合成了两个包含N-（叔丁基）苯并肼亚结构的N-吡啶基吡唑衍生物系列。它们对东方粘虫（Mythimna separata）和小菜蛾（Plutella xylostella）具有杀虫活性。）进行了评估。初步的生物测定结果表明，某些新化合物对东方粘虫和小菜蛾具有良好的杀虫活性。这些化合物的作用方式已通过钙显像技术进行了验证，结果表明，一些新化合物可以有效调节昆虫胞浆中的Ca ²⁺水平，并破坏细胞内钙稳态，表明其中某些化合物是该化合物的有效激活剂。 RyRs。

更新日期：2019-04-30

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