State Key Laboratory of Elemento-Organic Chemistry, College of Chemistry, Nankai University, Tianjin, China.
Key Laboratory of Study and Discovery of Small Targeted Molecules of Hunan Province, School of Medicine, Hunan Normal University, Changsha, China.
J Enzyme Inhib Med Chem. 2022 Dec;37(1):641-651. doi: 10.1080/14756366.2022.2032687.
To discover new agrochemicals with prominent pesticidal properties, a series of novel -naphthol derivatives containing benzothiazolylamino and various heteroaryl groups () were efficiently synthesised Betti reaction. The bioassay results showed that most of the synthesised compounds exhibited favourable insecticidal potentials, particularly towards oriental armyworm (50-100% at 200 mg·L) and diamondback moth (50-95% at 10 mg·L). Compounds , , , , , , and possessed LC values of 0.0988-5.8864 mg·L against diamondback moth. Compounds , , and also displayed lethality rates of 30-90% against spider mite at the concentration of 100 mg·L. Overall, some compounds could be considered as new insecticidal/acaricidal leading structures for further investigation. The calcium imaging experiments revealed that , , and could activate the release of calcium ions in insect () central neurons at a higher concentration (50 mg·L). The SAR analysis provided valuable information for further structural modifications.
为了发现具有显著农药性能的新农用化学品，我们通过 Bett 反应高效合成了一系列含有苯并噻唑基氨基和各种杂芳基的新型萘酚衍生物（）。生物测定结果表明，大多数合成化合物表现出良好的杀虫活性，特别是对东方粘虫（200mg·L 时 50-100%）和小菜蛾（10mg·L 时 50-95%）。化合物、、、、、、和对小菜蛾的 LC 值分别为 0.0988-5.8864mg·L。化合物、和在 100mg·L 浓度下对红蜘蛛也表现出 30-90%的致死率。总的来说，一些化合物可以被认为是进一步研究的新的杀虫/杀螨先导结构。钙成像实验表明，化合物、和在较高浓度（50mg·L）下能够激活昆虫（）中枢神经元释放钙离子。SAR 分析为进一步的结构修饰提供了有价值的信息。
