基于具有潜在杀线虫活性的托烷衍生物结构,通过1,3-偶极环加成反应,设计合成了19个未见报道的8-氮杂双环[3.2.1]辛烷-3-异噁唑肟类衍生物,通过^1H NMR,13C NMR和高分辨质谱对目标化合物的结构进行表征.初步的生物活性测试表明:在浓度25 mg/L下,目标化合物对南方根结线虫表现出良好的抑制活性,活性最好的化合物8-甲基-8-氮杂双环[3.2.1]辛烷-3-酮-O-((3-(4-硝基苯基)-4,5-二氢异噁唑-5-基)甲基)肟(9e)在1 mg/L浓度下对根结线虫的抑制率达55.6%.
Based on the potential nematicidal activities of tropane derivatives structure, 19 unreported 8-azabicyclo[3.2.1]-octane-3-isoxazole oxime derivatives were designed and synthesized by 1,3-dipolar cycloaddition reaction. Their structures were confirmed by 1H NMR, 13 C NMR and HRMS techniques. Preliminary bioassay results showed that targeted compounds exhibited good nematicidal activities against Meloidogyne incognita at concentration of 25 mg/L, and 8-methyl-8-azabicyclo-[3.2.1]octan-3-one-O-((3-(4-nitrophenyl)-4,5-dihydroisoxazol-5-yl)methyl)oxime(9e) showed the best nematicidal activities with 55.6% at concentration of 1 mg/L.