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

doi:10.6023/cjoc201712026

Chin. J. Org. Chem. ›› 2018, Vol. 38 ›› Issue (7): 1673-1679.DOI: 10.6023/cjoc201712026 Previous Articles Next Articles

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6-取代-吡啶并[3,2-e] [1,2,4]三唑并[4,3-a]吡嗪类衍生物的合成及抗惊厥活性研究

李佳丽^a, 胡涛^a, 张洪健^a, 宫国华^b,c, 全哲山^a

a 延边大学药学院延吉 133002;
b 内蒙古自治区蒙药心脑血管药理学重点实验室通辽 028000;
c 内蒙古民族大学附属医院通辽 028000

收稿日期:2017-12-18 修回日期:2018-02-02 发布日期:2018-04-12
通讯作者: 宫国华, 全哲山 E-mail:zsquan@ybu.edu.cn;gongguohua0211@163.com
基金资助:
国家自然科学基金（Nos.21662036，81660837）资助项目.

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

Received:2017-12-18 Revised:2018-02-02 Published:2018-04-12
Contact: 10.6023/cjoc201712026 E-mail:zsquan@ybu.edu.cn;gongguohua0211@163.com
Supported by:
Project supported by the National Natural Scicence Foundation of China (Nos. 21662036, 81660837).

1. Synthesis and Anticonvulsant Activity Evaluation of 6-Substituted-pyrido[3,2-e] [1,2,4]triazolo[4,3-a]pyrazine Derivatives.PDF(2650KB)

Abstract

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

Cite this article

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]. Chin. J. Org. Chem., 2018, 38(7): 1673-1679.

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6-取代-吡啶并[3,2-e] [1,2,4]三唑并[4,3-a]吡嗪类衍生物的合成及抗惊厥活性研究

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

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