化学学报 ›› 1999, Vol. 57 ›› Issue (5): 522-526. 上一篇    下一篇

研究论文

石杉碱甲类拟物的合成及药理研究1: (±)-14-氟石杉碱甲

曾繁星;蒋华良;杨玉社;刘东祥;陈建忠;唐希灿;刘静;沈竞康;陈凯先 ;嵇汝运   

  1. 中国科学院上海药物研究所.上海(200031)
  • 发布日期:1999-05-15

Syntheses and pharmacological studies of huperzine A analogues 1: ( ±)-14-fluorohuperzine A

Zeng Fanxing;Jiang Hualiang;Yang Yushe;Liu Dongxiang;Chen Jianzhong;Tang Xican;Liu Jing;Shen Jingkang;Chen Kaixian;Ji Ruyun   

  1. Shanghai Inst Mat Med., CAS.Shanghai(200031)
  • Published:1999-05-15

用两种方法合成了(±)-14-氟石杉碱甲(6),并测定了其抑制乙酰胆碱酯酶的生物活性。其抑制活性是(-)-石杉碱甲(1)的1/62。

关键词: 氟石杉碱甲, 氟化, 乙酰胆碱酯酶, 生物活性, 抑制剂, 老年性痴呆

The synthesis of (±)-14-fluorohuperzine A (6) has been accomplished and the activity of this agent to inhibit the activity of acetylcholinesterase has been measured. Taking into account its racemic form, this compound is 62 times less potent than that of natural (-)-huperzine A.

Key words: FLUORINATION, ACETYLCHOLINESTERASE, BIOLOGICAL ACTIVITY, INHIBITOR, SENILE DEMENTIA

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