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Synthesis and insecticidal activities of meta-diamide compounds containing an ethyl group
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DOI：10.1016/j.tetlet.2026.155985.png)
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Abstract
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In order to discover new, highly efficient and safe insecticides or insecticidal lead compounds, a series of metadiamide compounds containing an ethyl group were designed and synthesized using the proposed methods by our research team. The N-ethylation reaction of amines was achieved using ethyl formate, CH3COOH and NaBH (AcO)3, and the reaction mechanism was also explored. The results of biological activity tests showed that some compounds exhibited excellent insecticidal efficacy against Tetranychus cinnabarinus, Mythimna separata, and Plutella xylostella, demonstrating highly effective broad-spectrum insecticidal activity. Both compounds 6j and 6k demonstrated 100% insecticidal activity against P. xylostella at 0.1 mg/L, which was comparable to that of cyproflanilide. Furthermore, compound 6a exhibited 100% insecticidal activity against T. cinnabarinus at 10.00 mg/L, which further expanded its insecticidal spectrum. Molecular docking studies were conducted on the metabolic molecules of cyproflanilide and compound 6a with receptor proteins. The results indicated that the metabolic molecules of cyproflanilide and compound 6a have different binding sites with the target receptor, which may be the reason for their different insecticidal effects and spectra. The new N-ethylation synthesis method and the results of molecular docking analysis could provide a valuable foundation for the subsequent development of new meta-diamide insecticides.
Keywords:
meta -Diamide
Insecticidal activity
N -ethylation
Molecular docking
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