Design, Synthesis and Anticonvulsant Activity Evaluation of 7-Substituted-4H-[1,2,4]triazino[3,4-a]phthalazin-4-one Derivatives

被引：13

作者：

Sun, Xian-Yu ^{[1
,2
]}

Guan, Li-Ping ^{[1
]}

Zhang, Lei ^{[1
]}

Wei, Cheng-Xi ^{[1
]}

Piao, Hu-Ri ^{[1
]}

Quan, Zhe-Shan ^{[1
,2
]}

机构：

[1] Yanbian Univ, Key Lab Organism Funct Factors Changbai Mt, Minist Educ, Yanji 133002, Jilin, Peoples R China

[2] Yanbian Univ, Coll Pharm, Yanji 133002, Jilin, Peoples R China

来源：

JOURNAL OF THE BRAZILIAN CHEMICAL SOCIETY | 2009年 / 20卷 / 05期

基金：

中国国家自然科学基金;

关键词：

triazino; phthalazine; anticonvulsant; neurotoxicity; ANTIEPILEPTIC DRUG DEVELOPMENT; AGENTS;

D O I：

10.1590/S0103-50532009000500004

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

In this study, a novel series of 7-substituted-4H-[1,2,4]triazino[3,4-a]phthalazin-4-one derivatives was synthesized as potential anticonvulsant agents. Their anticonvulsant activities were evaluated by the maximal electroshock (MES) test, and their neurotoxicities were evaluated by the rotarod neurotoxicity test. The pharmacological results showed that 7-hexyloxy-4H-[1,2,4] triazino[3,4-a] phthalazin-4-one 4e was the most potent with median effective dose (ED50) value of 6.6 mg kg(-1), median toxicity dose (TD50) of 39.4 mg kg(-1), providing a protective index (PI=TD50/ED50) value of 6.0.

引用

页码：826 / 831

页数：6

共 13 条

[1] Synthesis and properties of new substituted 1,2,4-triazoles: Potential antitumor agents [J].