Vectorizing Pro-Insecticide: Influence of Linker Length on Insecticidal Activity and Phloem Mobility of New Tralopyril Derivatives

文献类型： 外文期刊

第一作者： Li, Tian Xing

作者： Li, Tian Xing;Chen, Yao;Liu, Hui Fang;Ma, Chi Yu;Yang, Wen

作者机构：

关键词： insecticide conjugate; glutamic acid; tralopyril; chlorfenapyr; phloem mobility

期刊名称：MOLECULES （ 影响因子：4.412； 五年影响因子：4.588 ）

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年卷期： 2021 年 26 卷 15 期

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收录情况： SCI

摘要： To improve the proinsecticidal activity and phloem mobility of amino acid-tralopyril conjugates further, nine conjugates were designed and synthesized by introducing glutamic acid to tralopyril, and the length of the linker between glutamic acid and tralopyril ranged from 2 atoms to 10 atoms. The results of insecticidal activity against the third-instar larvae of P. xylostella showed that conjugates 42, 43, 44,and 45 (straight-chain containing 2-5 atoms) exhibited good insecticidal activity, and their LC50 values were 0.2397 +/- 0.0366, 0.4413 +/- 0.0647, 0.4400 +/- 0.0624, and 0.4602 +/- 0.0655 mM, respectively. The concentrations of conjugates 43-45 were higher than that of conjugate 42 in the phloem sap at 2 h, and conjugate 43 showed the highest concentration. The introduction of glutamic acid can improve phloem mobility. The in vivo metabolism of conjugates 42 and 43 was investigated in P. xylostella, and the parent compound tralopyril was detected at concentrations of 0.5950 and 0.3172 nmol/kg, respectively. According to the above results, conjugates 42 and 43 were potential phloem mobile pro-insecticide candidates.

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