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Updated: Aug 13, 2026

Crystal Structure of the N-terminal Domain of Ryanodine Receptor from Plutella xylostella
Published on: November 30, 2018
Discovery of Substituted N-Arylindole Diamides as Insecticidal Candidates Targeting Ryanodine Receptor
Jiaying Duan1, Fengyu Li1, Changxu Lu1
1MARA Key Laboratory of Sustainable Crop Production in the Middle Reaches of the Yangtze River (Co-Construction by Ministry and Province)/Hubei Key Laboratory of Waterlogging Disaster and Agricultural Use of Wetland, College of Agriculture, Yangtze University, Jingzhou434025, P. R. China.
None:
Natural products are important sources of bioactive fragments. Based on the scaffold-hopping strategy, 40 novel N-arylindole diamide derivatives with excellent insecticidal activity were synthesized by substituting the pyrazole moiety of chlorantraniliprole (CHL) with a natural indole substructure. Bioassay results demonstrated that compound I ai exhibited a slightly higher LC50 value (LC50 = 0.26 mg·L-1) compared to CHL (LC50 = 0.11 mg·L-1) against Mythimna separata. For Plutella xylostella, compounds I an (LC50 = 1.74 × 10-2 mg·L-1) and I ah (LC50 = 2.19 × 10-2 mg·L-1) showed the same level of biological activity as CHL (LC50 = 8.6 × 10-3 mg·L-1). Mechanism validation experiment revealed that compound I ai could activate the insect ryanodine receptor to induce calcium ion release. Molecular docking, density functional theory calculations, and toxicity assays against Danio rerio validated its biosafety profile. These results will provide important guidance for the discovery of indole-containing diamide insecticides.
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