Synthesis and insecticidal activity study of novel anthranilic diamides analogs containing a diacylhydrazine bridge as effective Ca2+ modulators,Chemical Biology & Drug Design

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Synthesis and insecticidal activity study of novel anthranilic diamides analogs containing a diacylhydrazine bridge as effective Ca2+ modulators
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2018-07-15 , DOI: 10.1111/cbdd.13349
Yunyun Zhou ₁ , Wei Wei ₂ , Liangliang Zhu ₁ , Yuxin Li ₃ , Zhengming Li ₃

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Anthranilic diamides is a class of insecticides target at ryanodine receptors (RyRs). To discover potent insecticides targeting at RyRs, a series of novel anthranilic diamides with a diacylhydrazine bridge were designed and synthesized. Their insecticidal activities were evaluated and a preliminary structure‐activity relationship (SAR) was summarized. In particular, compound 5g exhibited good lethality against oriental armyworm (Mythimna separata) at a concentration of 5 mg/L. The calcium imaging experimental results indicated that the compound 5g can serve as effective insect Ca²⁺ level modulators by disrupting the cellular calcium homeostasis in Mythimna separata (Walker) and Spodoptera exigua (Hübner), which probably activated the RyRs on the ER membrane.

中文翻译：

新型的以二酰基肼桥为有效Ca 2+调节剂的邻氨基苯甲酰胺二酰胺类似物的合成和杀虫活性的研究

邻氨基苯甲酰胺是一类针对ryanodine受体（RyRs）的杀虫剂。为了发现针对RyRs的有效杀虫剂，设计并合成了一系列带有二酰基肼桥的新型邻氨基苯甲酰胺。对它们的杀虫活性进行了评估，并总结了初步的构效关系（SAR）。尤其是，化合物5g在浓度为5 mg / L时对东方粘虫（Mythimna separata）表现出良好的杀伤力。钙成像实验结果表明，化合物5g通过破坏Mythimna separata（Walker）和Mythimna separata（Walker）中的钙动态平衡，可作为有效的昆虫Ca ²⁺水平调节剂。Spodoptera exigua（Hübner），可能激活了ER膜上的RyRs。

更新日期：2018-07-15

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