Synthesis and Anticonvulsant Activities of 4-Alkoxyl-[1,2,4]Triazolo[4,3-a]Quinoxaline Derivatives

被引：0

作者：

Ren, Yang ^{[1
]}

Shen, Qing-Kun ^{[1
]}

Ding, Ming-Ming ^{[1
]}

Yin, Xiu-Mei ^{[1
]}

Quan, Zhen-Shan ^{[1
]}

机构：

[1] Yanbian Univ, Key Lab Nat Resources & Funct Mol Changbai Mt, Coll Pharm, Affiliated Minist Educ, Yanji 133002, Jilin, Peoples R China

来源：

LATIN AMERICAN JOURNAL OF PHARMACY | 2016年 / 35卷 / 10期

基金：

中国国家自然科学基金;

关键词：

anticonvulsant; maximal electroshock; neurotoxicity; quinoxaline; synthesis; triazole; ANTIEPILEPTIC DRUG DEVELOPMENT; DESIGN;

D O I：

暂无

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

In this paper, we described the syntheses and anticonvulsant activities of 4-alkoxyl-[1,2,4] triazolo[ 4,3-a] quinoxaline derivatives. The target compounds were screened for their anticonvulsant activities and neurotoxicities by maximal electroshock (MES) and rotarod tests, respectively. Among these compounds, 4-(pentyloxy)-[ 1,2,4] triazolo[4,3-a] quinoxaline (6r) was found by intraperitoneal administration in mice to be the most potent compound with a median effective dose (ED50) value of 27.4 mg/kg and a high protective index (PI) value of 5.7. The results demonstrated that compound 6r possessed better anticonvulsant activity and safer than the marketed drug valproate.

引用

页码：2169 / 2175

页数：7

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