Citation: Zhang Haiming, Zhang Hongjian, Tian Yushun, Quan Zheshan. Synthesis and Anticonvulsant Activity Evaluation of Phthalazine and Heterocyclic Derivatives[J]. Chinese Journal of Organic Chemistry, ;2017, 37(9): 2322-2327. doi: 10.6023/cjoc201703019 shu

Synthesis and Anticonvulsant Activity Evaluation of Phthalazine and Heterocyclic Derivatives

College of Pharmacy, Yanbian University, Yanji 133002

Corresponding author: Tian Yushun, ld-l@163.com
Received Date: 2 March 2017
Revised Date: 30 March 2017
Available Online: 10 September 2017
Fund Project: Project supported by the National Natural Science Foundation of China (No. 21272005)National Natural Science Foundation of China 21272005

Figures(1)

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.
- phthalazine,
- triazolo,
- tetrazolo,
- synthesis,
- anticonvulsant,
- the maximal electroshock
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