在这项研究中,旨在开发具有潜在生物活性的新型吡唑肟醚衍生物,32吡唑肟醚,包括取代的吡啶环,已经合成并通过1HNMR进行了结构鉴定,13CNMR,和HRMS。生物测定数据表明,这些化合物中的大多数对Mythimnaseparata具有很强的杀虫特性,灰心四虫,小菜蛾,以500μg/mL的剂量,一些标题化合物在500μg/mL时对Nilapavatalugens具有活性。此外,一些设计的化合物对M.separata具有有效的杀虫作用,T.Cinnabarinus,或100μg/mL的A.medicaginis,随着化合物8a的死亡率,8c,8d,8e,8f,8g,8o,8s,8v,8x,8z对抗A.medicaginis,特别是,全部达到100%。即使剂量降低到20μg/mL,化合物8s还对分离分枝杆菌表现出50%的杀虫活性,和化合物8a,8e,8f,8o,8v,8x对A.medicaginis的抑制率超过60%。目前的研究结果为未来生物活性吡唑肟醚的合理设计提供了重要的依据。
In this research, with an aim to develop novel pyrazole oxime ether derivatives possessing potential biological activity, thirty-two pyrazole oxime ethers, including a substituted pyridine ring, have been synthesized and structurally identified through 1H NMR, 13C NMR, and HRMS. Bioassay data indicated that most of these compounds owned strong insecticidal properties against Mythimna separata, Tetranychus cinnabarinus, Plutella xylostella, and Aphis medicaginis at a dosage of 500 μg/mL, and some title compounds were active towards Nilaparvata lugens at 500 μg/mL. Furthermore, some of the designed compounds had potent insecticidal effects against M. separata, T. cinnabarinus, or A. medicaginis at 100 μg/mL, with the mortalities of compounds 8a, 8c, 8d, 8e, 8f, 8g, 8o, 8s, 8v, 8x, and 8z against A. medicaginis, in particular, all reaching 100%. Even when the dosage was lowered to 20 μg/mL, compound 8s also expressed 50% insecticidal activity against M. separata, and compounds 8a, 8e, 8f, 8o, 8v, and 8x displayed more than 60% inhibition rates against A. medicaginis. The current results provided a significant basis for the rational design of biologically active pyrazole oxime ethers in future.