有机化学 ›› 2017, Vol. 37 ›› Issue (9): 2322-2327.DOI: 10.6023/cjoc201703019 上一篇    下一篇

研究论文

酞嗪并三唑或四唑类衍生物的合成及其抗惊厥活性研究

张海明, 张洪健, 田玉顺, 全哲山   

  1. 延边大学药学院 延吉 133002
  • 收稿日期:2017-03-02 修回日期:2017-03-30 出版日期:2017-09-25 发布日期:2017-05-17
  • 通讯作者: 田玉顺 E-mail:ld-l@163.com
  • 基金资助:

    国家自然科学基金(No.21272005)资助项目.

Synthesis and Anticonvulsant Activity Evaluation of Phthalazine and Heterocyclic Derivatives

Zhang Haiming, Zhang Hongjian, Tian Yushun, Quan Zheshan   

  1. College of Pharmacy, Yanbian University, Yanji 133002
  • Received:2017-03-02 Revised:2017-03-30 Online:2017-09-25 Published:2017-05-17
  • Contact: 10.6023/cjoc201703019 E-mail:ld-l@163.com
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No. 21272005).

设计合成了6-取代-1,2,4-三氮唑并[3,4-a]酞嗪和6-取代四氮唑并[5,1-a]酞嗪四个系列16个衍生物.其化学结构均经过1H NMR、13C NMR、IR和HRMS确征.药理方面,利用最大电惊厥法(MES),以小鼠腹腔给药测定其抗惊厥活性.实验结果显示N-(4-溴苯基)-四唑[5,1-a]酞嗪-6-胺(7a)的抗惊厥活性最强,其半数有效量ED50为5.89 mg·kg-1,抗惊厥作用强于对照药卡马西平.

关键词: 酞嗪, 三唑, 四唑, 合成, 抗惊厥, 最大电惊厥法

Four series of derivatives, 6-substituted-1,2,4-triazolo[3,4-a] phthalazine derivatives and 6-substituted tetrazolo[5,1-a]phthalazine derivatives have been synthesized. The structures of compounds are confirmed by 1H NMR, 13C NMR, IR and HRMS. The anticonvulsant effects of the compounds are evaluated with maximal electroshock test by intraperitoneally injected in mice. The experimental results show that N-(4-bromophenyl)tetrazolo[5,1-a]phthalazin-6-amine (7a) was the most potent compound, with a median effective dose of 5.89 mg·kg-1. Its anticonvulsant effect is better than the reference drug, carbamazepine.

Key words: phthalazine, triazolo, tetrazolo, synthesis, anticonvulsant, the maximal electroshock