Citation: 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 shu

Synthesis and Anticonvulsant Activity Evaluation of 6-Substituted-pyrido[3, 2-e] [1, 2, 4]triazolo[4, 3-a]pyrazine Derivatives

Li Jiali ^a ,
Hu Tao ^a ,
Zhang Hongjian ^a ,
Gong Guohua ^b,c,, ,
Quan Zhe-Shan ^a,,

a.
College of Pharmacy, Yanbian University, Yanji 133002
b.
Inner Mongolia Autonomous Region Key laboratory of Mongolian Medicine Pharmacology for Cardio-cerebral Vascular System, Tongliao 028000
c.
Affiliated Hospital of Inner Mongolia University for Nationalities, Tongliao 028000

Corresponding author: Gong Guohua, gongguohua0211@163.com Quan Zhe-Shan, zsquan@ybu.edu.cn
Received Date: 18 December 2017
Revised Date: 2 February 2018
Available Online: 12 July 2018
Fund Project: the National Natural Scicence Foundation of China 21662036the National Natural Scicence Foundation of China 81660837Project supported by the National Natural Scicence Foundation of China (Nos. 21662036, 81660837)

Figures(2)

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.
- pyrido[2, 3-b]pyrazine,
- triazole,
- synthesis,
- anticonvulsant,
- the maximal electroshock
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