文献类型：期刊文献

英文题名：Diamides conformationally restricted with central amino acid: Design, synthesis, and biological activities

作者：Chen, Rui-Jia[1];Zhou, Cong[1];Dong, Le-Feng[1];Feng, Ting-Ting[1];Wang, Gang-Ao[1];Wang, Jun-Jie[1];Gu, Yu-Cheng[2];Xu, Zhi-Ping[1];Cheng, Jia-Gao[1];Shao, Xu-Sheng[1];Xu, Xiao-Yong[1];Li, Zhong[1]

机构：[1]East China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab Chem Biol, Shanghai 200237, Peoples R China;[2]Syngenta, Jealotts Hill Int Res Ctr, Bracknell, Berks, England

年份：2022

卷号：59

期号：6

起止页码：1045

外文期刊名：JOURNAL OF HETEROCYCLIC CHEMISTRY

收录：;WOS:【SCI-EXPANDED(收录号:WOS:000747763400001)】；

基金：National Key Research and Development Program of China, Grant/Award Number: 2017YFD0200500

语种：英文

摘要：Diamide insecticides, represented by chlorantraniliprole (CHL), were widely applied in the control of lepidopteran insects. In efforts to develop bioactive diamides with novel scaffolds, we design and synthesized a series of diamides containing central amino acids to conformationally simulate CHL. Bioassay results indicated that most compounds containing 1-aminocyclopropane-1-carboxylic acid exhibited excellent larvacidal potency against Mythimna separate and Plutella xylostella. After a systematic structure-activity relationship study, 1-23 was identified as a potential insecticidal candidate with LC50 values of 34.920 mg center dot L-1 against M. separate and 61.992 mg center dot L-1 on P. xylostella. Finally, molecular docking revealed the possible binding mode of 1-23 with the target protein, ryanodine receptors.