Red de Estudios Moleculares Avanzados, Clúster Científico y Tecnológico BioMimic, Campus III, Instituto de Ecología, A.C. Carretera Antigua a Coatepec 351, 91073 Xalapa, Veracruz México.
Cátedra CONACyT en el, Instituto de Ecología AC, Xalapa Veracruz México.
J Agric Food Chem. 2021 Feb 10;69(5):1455-1465. doi: 10.1021/acs.jafc.0c05997. Epub 2021 Jan 26.
In this research, six neonicotinoid analogs derived from l-proline were synthesized, characterized, and evaluated as insecticides against . Most of the target compounds showed good to excellent insecticidal activity. To the best of our knowledge, this is the first report dealing with the use of enantiopure l-proline to get neonicotinoids. These results highlighted the compound as an excellent candidate used as the lead chiral insecticide for future development. Additionally, molecular docking with the receptor and compound was carried out to gain insight into its high activity when compared to dinotefuran. Finally, the neurotoxic evaluation of compound showed lower toxicity than the classic neonicotinoid dinotefuran.
在这项研究中，合成了六种源自 l-脯氨酸的新烟碱类似物，并对其进行了鉴定和评估，作为杀虫剂来防治 。大多数目标化合物表现出良好到优异的杀虫活性。据我们所知，这是首次报道使用手性纯 l-脯氨酸来获得新烟碱类杀虫剂。这些结果突出了化合物 作为一种优秀的候选物，可作为未来开发的先导手性杀虫剂。此外，还进行了与受体和化合物的分子对接，以深入了解其与噻虫嗪相比的高活性。最后，化合物 的神经毒性评估显示其毒性低于经典的新烟碱类杀虫剂噻虫嗪。
