Synthesis and anticonvulsant activity of 7-alkoxyl-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinolines

被引：89
作者：
Xie, ZF
Chai, KY
Piao, HR
Kwak, KC
Quan, ZS [1 ]
机构：
[1] Yanbian Univ, Coll Pharm, Yanji 133000, Jilin, Peoples R China
[2] Wonkwang Univ, Dept Chem, Iksan 570749, South Korea
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 21期
基金：
中国国家自然科学基金;
关键词：
1,2,4]triazolo[4,3-a]quinolines; anticonvulsant; maximal electroshock; pentylenetetrazol; neurotoxicity;
D O I：
10.1016/j.bmcl.2005.07.051
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of 7-alkoxyl-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinoline derivatives was synthesized using 6-hydroxy-3,4-dihydro- 1H-quinolin-2-one as a starting material. Their anticonvulsant activities were evaluated by the maximal electroshock test (MES test) and the subcutaneous (sc) pentylenetetrazol test (scMet test), and their neurotoxicity was evaluated by the rotarod neurotoxicity test (Tox). MES and scMet tests show that 7-(4-fluorobenzyloxy)-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinoline 41 was found to be the most potent with ED50 value of 11.8 and 6.7 mg kg(-1) and protective index (PI = TD50/ED50) value of 4.6 and 8.1, respectively. (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码：4803 / 4805
页数：3
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