Zhang Chiying, Tian Qingqiang, Li Yahui
Key Laboratory of Agri-Food Safety of Anhui Province, School of Resources and Environment, Anhui Agricultural University, Hefei, China.
State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bio-engineering, Ministry of Education, Guizhou University, Guiyang, China.
Front Chem. 2022 Jul 26;10:973630. doi: 10.3389/fchem.2022.973630. eCollection 2022.
Structural optimization of natural products has become one of the most effective ways to develop novel pesticides. In this study, 30 novel pesticide derivatives containing a linear bisamide were synthesized. Then, their insecticidal activities against were evaluated. Results indicate that different bisamide substitutes show different larvicidal structure-activity relationships. At the same time, 2-trifluoroethyl is the most efficient substituent. The bioactivity results showed that most of the desired compounds exhibited better insecticidal activity against than piperine. Among them, resulted in 90% mortality at 1 mg/ml concentration. This study provides a novel protocol for the discovery of new insecticides. The molecular docking results indicated that compound D28 could act on -aminobutyric acid receptors.
天然产物的结构优化已成为开发新型农药最有效的方法之一。在本研究中，合成了30种含线性双酰胺的新型农药衍生物。然后，评估了它们对……的杀虫活性。结果表明，不同的双酰胺取代基呈现出不同的杀幼虫构效关系。同时，2-三氟乙基是最有效的取代基。生物活性结果表明，大多数目标化合物对……表现出比胡椒碱更好的杀虫活性。其中，……在1mg/ml浓度下导致90%的死亡率。本研究为新型杀虫剂的发现提供了一种新方案。分子对接结果表明，化合物D28可作用于γ-氨基丁酸受体。
