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[α-(2-氧代烷基)-α-(取代苯胺基)甲基苯基]-β-D-吡喃阿洛糖苷的合成及镇静活性研究
引用本文:祝钱莉,唐强,李颖,尹述凡.[α-(2-氧代烷基)-α-(取代苯胺基)甲基苯基]-β-D-吡喃阿洛糖苷的合成及镇静活性研究[J].有机化学,2006,26(9):1264-1267.
作者姓名:祝钱莉  唐强  李颖  尹述凡
作者单位:四川大学化学学院,成都,610064
基金项目:致谢本论文的镇静活性实验由四川大学药学院药理教研室包旭老师等完成,在此表示衷心的感谢.
摘    要:以豆腐果苷为原料, 通过Mannich反应与取代苯胺和脂肪酮共合成了七个豆腐果苷衍生物, 均未见文献报道. 其结构经1H NMR, IR, MS和HRMS确认, 并进行了药理活性筛选. 结果表明, 部分化合物均具有良好的镇静活性. 其中, 化合物2a (200 mg/kg), 2b (200 or 100 mg/kg)和2e (200 mg/kg)与豆腐果苷相比较, 具有更强的疗效.

关 键 词:豆腐果苷  Mannich碱  合成  镇静活性
收稿时间:12 6 2005 12:00AM
修稿时间:03 6 2006 12:00AM

Synthesis and Calm Activity of [α-(2-Oxoalkyl)-α-(substituted Anilimo ) methyl] phenyl-β- D-allopyranoside
ZHU Qian-Li,TANG Qiang,LI Ying,YIN Shu-Fan.Synthesis and Calm Activity of [α-(2-Oxoalkyl)-α-(substituted Anilimo ) methyl] phenyl-β- D-allopyranoside[J].Chinese Journal of Organic Chemistry,2006,26(9):1264-1267.
Authors:ZHU Qian-Li  TANG Qiang  LI Ying  YIN Shu-Fan
Institution:Faculty of Chemistry, Sichuan University, Chengdu 610064
Abstract:Seven novel helicid derivatives have been designed and synthesized by the Mannich reaction of helicid with substituted aniline and aliphatic ketone. The structures of all these new compounds were char- acterized by 1H NMR, IR, MS and HRMS spectra. The preliminary bioassay test suggested that some of such compounds should show good calm activity. For example, compounds 2a (200 mg/kg), 2b (200 or 100 mg/kg) and 2e (200 mg/kg) are more effective than the parent helicid.
Keywords:helicide  Mannich base  synthesis  calm activity
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