Chin. J. Org. Chem. ›› 2017, Vol. 37 ›› Issue (9): 2322-2327.DOI: 10.6023/cjoc201703019 Previous Articles     Next Articles



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 发布日期:2017-05-17
  • 通讯作者: 田玉顺
  • 基金资助:


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 Published:2017-05-17
  • Contact: 10.6023/cjoc201703019
  • Supported by:

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

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