Abstract
Increasing the diversity of lead compounds has been shown to enhance the efficacy of diamide insecticides. Fifty novel compounds were precisely designed and synthesized utilizing fragment-based assembly and virtual screening coupling. The median lethal concentration (LC50) values of compounds X-30 and X-40 against Mythimna separata were 0.09 and 0.08 mg L-1, respectively, which are lower than that of chlorantraniliprole (CHL, 0.11 mg L-1). Notably, compounds X-10, X-18, X-25, X-32 and X-43 had corresponding LC50 values of 2.0 × 10-4, 5.0 × 10-4, 6.0 × 10-4, 9.0 × 10-4 and 7.0 × 10-4 mg L-1 against Plutella xylostella, respectively. The best compound X-10 exhibited five-fold greater efficacy than CHL (1.0 × 10-3 mg L-1). The LC50 values of compounds X-21, X-29, and X-40 against Spodoptera frugiperda were 0.27, 0.26 and 0.25 mg L-1, respectively, which are slightly lower than that of CHL (0.33 mg L-1). In the case of Ostrinia furnacalis, compound X-43 showed good efficacy with LC50 values comparable to those of CHL (1.38 versus 1.57 mg L-1). Calcium imaging experiments demonstrated that X-21 acted on S. frugiperda ryanodine receptors. Furthermore, this series of compounds showed safety toward nontarget mammals compared to CHL. The introduction of fluorinated alkoxy groups at the 3-position of the pyrazole ring leads to good insecticidal activity and improved insect selectivity. © 2025 Society of Chemical Industry.
Published Version
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