当前位置: X-MOL 学术Bioorg. Med. Chem. Lett. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Synthesis, Biological Activities, and SAR Studies of Novel 1-(2-chloro-4,5-difluorophenyl)-1H-pyrazole Derivatives.
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2020-09-06 , DOI: 10.1016/j.bmcl.2020.127535
Yangyang Zhao 1 , Huangong Li 1 , Pengwei Sun 1 , Li Gao 1 , Jingbo Liu 1 , Sha Zhou 1 , Lixia Xiong 1 , Na Yang 1 , Yuxin Li 1 , Zhengming Li 1
Affiliation  

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−1, equivalent to that of chlorantraniliprole (36%, 0.1 mg L−1). The activity of IVc against Plutella xylostella was 90% at 10-5 mg L−1, 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.



中文翻译:

新型1-(2-氯-4,5-二氟苯基)-1H-吡唑衍生物的合成,生物活性和SAR研究。

为了寻找新的ryanodine受体(RyR)调节剂,设计了一系列35种新的含氟取代化合物,它们引入了含有修饰的吡唑杂环的1-(2-氯-4,5-二氟苯基)-1 H-吡唑部分,并合成的。然后,测试了它们对我们温室中的Mythimna separataPlutella xylostella的杀虫活性。经过系统的生物学筛选后,发现IVc在0.1 mg L -1时显示出对分离出的Mythimna separata的杀幼虫活性为50%,相当于毒死ili(36%,0.1 mg L -1)。IVc小菜蛾的活性在10 -5 mg L -1时为90%,而在相同浓度下,四氢氯氰菊酯为70%。然后,进行昆虫电生理实验以研究IVcIVe的作用模式。实验结果证实,这两种化合物均可以导致神经元内质网中钙的释放,成为经典的邻氨基苯甲酰胺类杀虫剂。

更新日期:2020-09-07
down
wechat
bug