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
收藏
页码：833 / 839
页数：7
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