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Updated: Jan 7, 2026
Crystal Structure of the N-terminal Domain of Ryanodine Receptor from Plutella xylostella
Published on: November 30, 2018
Novel amide derivatives containing acylthiourea link targeting insect ryanodine receptors: Design, synthesis,
Weibin Xie1, Hongyuan Zhang1, Wei Wei1
1State Key Laboratory of Elemento-Organic Chemistry, Department of Chemistry, Nankai University, 94 Weijin Road, Tianjin, 300071, China.
Abstract:
Diamide insecticides targeting insect ryanodine receptors (RyRs) have been widely used for pest control, but have faced growing challenges from resistance driven by RyR mutations. To address this issue, 22 novel amide derivatives containing acylthiourea linkages were designed through fragment-based splicing, and their insecticidal activity against Mythimna separata (M. separata) and Spodoptera frugiperda (S. frugiperda) was evaluated. Compound 9a exhibited the highest efficacy against M. separata (40 % lethality at 0.5 mg/L). Time-lapse [Ca2+]ER measurements showed that 9a was active against wild-type S. frugiperda RyR(SfRyR) but inactive against rabbit RyR1. Meanwhile, 3D-QSAR model analysis identified the steric field as the dominant factor influencing activity, and molecular docking, dynamics simulations, and binding free energy calculations confirmed stable binding to both wild-type and resistant (G4891E/I4734M mutant) SfRyR. These findings offer a reference for guiding the rational design of RyR-targeted amide insecticides.
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