Synthesis of novel 7-benzylamino-2H-1,4-benzoxazin-3(4H)-ones as anticonvulsant agents

被引：28
|
作者：
Piao, Zhong-Tai [1 ,2 ]
Guan, Li-Ping [1 ]
Zhao, Li-Ming [1 ]
Piao, Hu-Ri [1 ]
Quan, Zhe-Shan [1 ,2 ]
机构：
[1] Yanbian Univ, Coll Pharm, Yanji 133000, Jilin Province, Peoples R China
[2] Yanbian Univ, Key Lab Organism Funct Factors Changbai Mt, Minist Educ, Yanji 133000, Jilin Province, Peoples R China
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2008年 / 43卷 / 06期
基金：
中国国家自然科学基金;
关键词：
1,4-benzoxazin-3(4H)-one; anticonvulsant; MES; sc-PTZ; isoniazid; strychnine;
D O I：
10.1016/j.ejmech.2007.08.006
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of 7-benzylamino-2H-1,4-benzoxazin-3(4H)-ones were synthesized using 2-amino-5-nitrophenol as a starting material. Their anticonvulsant activities were evaluated by the maximal electroshock test (MES test) and their neurotoxicity was evaluated by the rotarod neurotoxicity test (Tox.). The MES test showed that 7-(4-fluorobenzylamino)-2H-1,4-benzoxazin-3(4H)-one 4b was the most potent with ED50 Value of 31.7 mg/kg and protective index (PI = TD50/ED50) value of 7.2. To explain the possible mechanism of anticonvulsant activity, the compound 4b was tested in sc-PTZ test, isoniazid test and strychnine test. (c) 2007 Published by Elsevier Masson SAS.
引用
收藏
页码：1216 / 1221
页数：6
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