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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 showed that conjugates , , ,and (straight-chain containing 2-5 atoms) exhibited good insecticidal activity, and their LC 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 - were higher than that of conjugate in the phloem sap at 2 h, and conjugate showed the highest concentration. The introduction of glutamic acid can improve phloem mobility. The in vivo metabolism of conjugates and was investigated in , and the parent compound tralopyril was detected at concentrations of 0.5950 and 0.3172 nmol/kg, respectively. According to the above results, conjugates and were potential phloem mobile pro-insecticide candidates.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8348000 | PMC |
| http://dx.doi.org/10.3390/molecules26154570 | DOI Listing |
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