Chinese Journal of Organic Chemistry >
Synthesis and Anticonvulsant Activity Evaluation of 6-Substituted-pyrido[3,2-e] [1,2,4]triazolo[4,3-a]pyrazine Derivatives
Received date: 2017-12-18
Revised date: 2018-02-02
Online published: 2018-04-12
Supported by
Project supported by the National Natural Scicence Foundation of China (Nos. 21662036, 81660837).
In this paper, a series of 6-substituted-pyrido[3,2-e] [1,2,4]triazolo[4,3-a]pyrazine derivatives have been synthesized. Their anticonvulsant activity and neurotoxicity in mice were evaluated by maximal electroshock (MES) and rotarod test, respectively. The structures were confirmed by 1H NMR, 13C NMR, MS and HRMS. The experimental results show that 6-phenoxypyrido[3,2-e] [1,2,4]triazolo[4,3-a]pyrazine (5g) was safer than the reference drug, carbamazepine, with ED50value of 93.9 mg·kg-1and protective index (PI) value of 24.3, which was a potential anti-epilepsy candidate compound.
Key words： pyrido[2,3-b]pyrazine; triazole; synthesis; anticonvulsant; the maximal electroshock
Li Jiali , Hu Tao , Zhang Hongjian , Gong Guohua , Quan Zhe-Shan . Synthesis and Anticonvulsant Activity Evaluation of 6-Substituted-pyrido[3,2-e] [1,2,4]triazolo[4,3-a]pyrazine Derivatives[J]. Chinese Journal of Organic Chemistry, 2018 , 38(7) : 1673 -1679 . DOI: 10.6023/cjoc201712026
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