Chinese Journal of Organic Chemistry >
Synthesis and Anticonvulsant Activity Evaluation of Phthalazine and Heterocyclic Derivatives
Received date: 2017-03-02
Revised date: 2017-03-30
Online published: 2017-05-17
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
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
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