State Key Laboratory of Molecular Engineering of Polymers, Department of Macromolecular Science, Fudan University, Yangpu District, Shanghai, China.
WuXi AppTec (Tian Jin) Co., Ltd., Tianjin, China.
Chem Biol Drug Des. 2018 Nov;92(5):1914-1919. doi: 10.1111/cbdd.13349. Epub 2018 Jul 15.
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 Ca 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.
邻苯二甲酰亚胺二酰胺类化合物是一类作用于肌浆网钙离子通道（RyRs）的杀虫剂。为了发现作用于 RyRs 的新型高效杀虫剂，设计并合成了一系列含有二酰肼桥的新型邻苯二甲酰亚胺二酰胺类化合物。对其杀虫活性进行了评价，并总结了初步的构效关系（SAR）。特别是化合物 5g 在 5mg/L 浓度下对东方粘虫（Mythimna separata）表现出良好的致死活性。钙成像实验结果表明，化合物 5g 通过破坏东方粘虫（Mythimna separata）和斜纹夜蛾（Spodoptera exigua）细胞内钙稳态，可作为有效的昆虫 Ca 水平调节剂，这可能激活内质网膜上的 RyRs。
