杂环或大位阻基团固定硝基位向的新型新烟碱类化合物的分子设计,合成及生物活性

摘要

Neonicotinoids,targeting insect nicotinic acetylcholine receptors (nAChRs),has attracted considerable attentions for decades.To explore the influence of configuration of-NO2 on bioactivities and search for compounds with higher activities,some classes of neonicotinoids containing tetrahydropyridine or bukyl substituent were synthesized,in which the -NO2 and pyridine was kept in same side of nitromethylene.Neonicotinoids with tetrahydropyridine fixed cis configuration exhibited high activities against cowpea aphids and brown planthopper (Nilaparvata lugens),furthermore,some compounds showed higher insecticidal activities against imidacloprid-resistant brown planthopper than imidacloprid.However,the open-chain analogues with tetrahydropyridine fixed cis configuration only exhibited some knockdown activities against cowpea aphids.Neonicotinoids with bulky substituents fixed cis configuration compounds exhibited higher insecticidal activities against cowpea aphids,armyworm and Nephotettix bipunctatus (Fabricius).