College of Plant Protection/Chemistry and Pharmacy, Northwest A&F University, Yangling 712100, Shaanxi Province, PR China.
College of Plant Protection/Chemistry and Pharmacy, Northwest A&F University, Yangling 712100, Shaanxi Province, PR China.
Bioorg Med Chem Lett. 2021 Jul 1;43:128104. doi: 10.1016/j.bmcl.2021.128104. Epub 2021 May 10.
To explore natural-product-based insecticide candidates, and high value-added application of natural plants in agriculture, a series of twin compounds were prepared from two natural products podophyllotoxin and cytisine, which are isolated from the plants Podophyllum hexandrum and Thermopsis lanceolata, respectively. Compounds IIa (X = Cl, Y = R = R = H), IIIc (X = Y = R = R = Cl) and IVd (X = R = R = Br, Y = H) exhibited >2-fold potent insecticidal activity of podophyllotoxin against armyworm with FMRs greater than 60%. SARs were also observed. It is noteworthy that the idea of twin insecticides was addressed for the first time. We hope this idea will be conducive to design new twin insecticidal agents, and lay the foundation for future high value-added application of the plants P. hexandrum and T. lanceolata as potentially botanical pesticides in agriculture.
为了探索基于天然产物的杀虫剂候选物，以及天然植物在农业中的高附加值应用，从两种天然产物鬼臼毒素和野靛碱中分别分离得到的植物八角莲和木蓝，分别合成了一系列孪生化合物。化合物 IIa（X=Cl，Y=R=R=H）、IIId（X=Y=R=R=Cl）和 IVd（X=R=R=Br，Y=H）对粘虫的杀虫活性比鬼臼毒素高 2 倍以上，FMR 大于 60%。还观察到了构效关系。值得注意的是，首次提出了双杀虫剂的概念。我们希望这个想法将有助于设计新的双杀虫剂，并为未来八角莲和木蓝作为潜在的植物性农药在农业中的高附加值应用奠定基础。
