Synthesis and Anticonvulsant Activity of Novel 3-(2-(4H-1,2,4-triazol-4-yl)ethyl)-1-alkyl-1H-indole Derivatives

被引：6

作者：

Liu, Chuan-Feng ^{[1
]}

Zhang, Hong-Jian ^{[1
]}

Quan, Zhe-Shan ^{[1
]}

机构：

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

来源：

Letters in Drug Design & Discovery | 2016年 / 13卷 / 08期

基金：

中国国家自然科学基金;

关键词：

Synthesis; anticonvulsant; triazole; indole; maximal electroshock; ANTIEPILEPTIC DRUG;

D O I：

10.2174/1570180813666160324173717

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel 3-[2-(4H-1,2,4-triazol-4-yl) ethyl]-1-alkyl-1H-indole derivatives (4a-s) were synthesized and evaluated for their anticonvulsant activity and neurotoxicity by using maximal electroshock (MES) and rotarod neurotoxicity (TOX) tests. Among the compounds studied, compound 3-[2-(4H-1,2,4-triazol-4-yl) ethyl]-1-nonyl-1H-indole (4p) was found by intraperitoneal (i.p.) administration in mice to be the most potent compound with a median effective dose (ED50) value of 10.2 mg/kg, possessed better anticonvulsant activity and higher safety than carbamazepine.

引用

页码：833 / 839

页数：7

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