Synthesis, Insecticidal Activities, and 3D-QASR of N-Pyridylpyrazole Amide Derivatives Containing a Phthalimide as Potential Ryanodine Receptor Activators

• DOI: 10.1021/acs.jafc.2c03971
• Publication Date: 2022-09-22T11:54:15Z
• Authors: Lu Zhang; Ruijia Chen; Xiaoyang Li; Xiaoyong Xu; Zhiping Xu; Jiagao Cheng; Yanli Wang; Yuxin Li; XuSheng Shao; Zhong Li
• Keywords: Mythimna separata; Amide; Lead compound

To develop potent and environment-friendly insecticides, novel N-pyridylpyrazole amide derivatives containing a phthalimide were designed synthesized. The preliminary bioassay results showed that most of the target compounds exhibited good insecticidal activities. For oriental armyworm (Mythimna separata), E5, E29, E30, E33 displayed higher than 90% lethal rates at 25 mg L-1. In particular, compound 60% mortality lower concentration 6.25 Besides, also 30% rate 5 L-1 against diamondback moth (DBM) (Plutella xylostella). Molecular docking between active DBM ryanodine receptor (RyR), comparative molecular field analysis (CoMFA), density functional theory (DFT) calculations conducted discussed. Furthermore, according to vitro studies using calcium imaging technique, was lead targeting insect RyR.