新型哌啶-4-醇衍生物的合成及生物活性  

Synthesis and biological activity of novel piperidin-4-ol derivatives

作　　者：孙海洋 杨晓宁 李晖 王佳毅[1] 宋恭华[1] SUN Haiyang;YANG Xiaoning;LI Hui;WANG Jiayi;SONG Gonghua(School of Pharmacy,East China University of Science and Technology,Shanghai Key Laboratory of Chemical Biology,Shanghai 200237,China)

机构地区：[1]华东理工大学药学院,上海市化学生物学重点实验室,上海200237

出　　处：《农药学学报》2023年第2期329-339,共11页Chinese Journal of Pesticide Science

基　　金：国家重点研发计划(2018YFD0200105).

摘　　要：发现具有新作用方式的农药对于现代作物保护至关重要。本研究以哌啶醇和邻苯二酚为起始原料,经5步反应制备得到了一系列新型的哌啶-4-醇衍生物,并通过核磁共振氢谱、碳谱和高分辨质谱确认其结构。生物活性测试结果表明,部分目标化合物在25 mg/L质量浓度下表现出良好的根结线虫Meloidogyne incognita抑制活性。此外,在500 mg/L质量浓度下,大部分化合物对黏虫Pseudaletia separata Walker表现出因拒食效应所致的体重减轻。The discovery of pesticides with novel mode of action is crucial for modern crop protection.In present work,a series of novel piperidin-4-ol derivatives were synthesized by 5-step reactions using piperidinol and catechol as starting materials.All target compounds were characterized by 1H NMR,13C NMR and HRMS.The biological activities of synthesized compounds were evaluated against Meloidogyne incognita and Pseudaletia separata Walker respectively.It was found that some target compounds exhibited good nematicidal activity against M.incognita at 25 mg/L.Obvious weight reduction on P.separata was also observed for most of the compounds at 500 mg/L due to their antifeeding effects on the armyworm.

关 键 词：哌啶-4-醇 杀线虫活性 黏虫 拒食效应 

分 类 号：O626.3[理学—有机化学] TQ459[理学—化学]