State Key Laboratory of Elemento-Organic Chemistry, Institute of Elemento-Organic Chemistry, Nankai University, Tianjin 300071, China.
State Key Laboratory of Elemento-Organic Chemistry, Institute of Elemento-Organic Chemistry, Nankai University, Tianjin 300071, China.
Bioorg Med Chem Lett. 2020 Nov 15;30(22):127535. doi: 10.1016/j.bmcl.2020.127535. Epub 2020 Sep 6.
In order to search for the new ryanodine receptor (RyR) regulator, a series of 35 novel fluoro-substituted compounds introduced 1-(2-chloro-4,5-difluorophenyl)-1H-pyrazole moiety containing modified pyrazole heterocycle were designed and synthesized. Then, they were tested for the insecticidal activities against Mythimna separata and Plutella xylostella in our greenhouse. After a systematic biological screening, it was found out that IVc showed 50% larvicidal activities against Mythimna separata at 0.1 mg L, equivalent to that of chlorantraniliprole (36%, 0.1 mg L). The activity of IVc against Plutella xylostella was 90% at 10 mg L, whereas the chlorantraniliprole was 70% at the same concentration. Then, insect electrophysiology experiments were conducted to study the pattern of action of IVc and IVe. It was confirmed by the experimental results that both compounds could lead to the release of calcium from the endoplasmic reticulum of neurons as classical anthranilic diamide insecticides.
为了寻找新型的ryanodine 受体（RyR）调节剂，设计并合成了一系列 35 种新型氟取代化合物，这些化合物引入了含有修饰吡唑杂环的 1-（2-氯-4,5-二氟苯基）-1H-吡唑部分。然后，在我们的温室中对它们对粘虫和小菜蛾的杀虫活性进行了测试。经过系统的生物筛选，发现 IVc 在 0.1mg/L 时对粘虫的 50%幼虫致死活性与氯虫苯甲酰胺（36%，0.1mg/L）相当。IVc 对小菜蛾的活性在 10mg/L 时为 90%，而氯虫苯甲酰胺在相同浓度下为 70%。然后，进行了昆虫电生理学实验来研究 IVc 和 IVe 的作用模式。实验结果证实，这两种化合物都可以像经典的邻苯二甲酰胺类杀虫剂一样，导致神经元内质网中的钙离子释放。
