SYNTHESIS AND ANTICONVULSANT ACTIVITY OF 2 N-(2,6-DIMETHYLPHENYL)PYRIDINEDICARBOXIMIDES

被引：5
|
作者：
BAILLEUX, V [1 ]
VALLEE, L [1 ]
NUYTS, JP [1 ]
VAMECQ, J [1 ]
机构：
[1] CHU LILLE,HOP B,CTR EPILEPSY,F-59037 LILLE,FRANCE
来源：
BIOMEDICINE & PHARMACOTHERAPY | 1995年 / 49卷 / 02期
关键词：
N-(2,6-DIMETHYLPHENYL)PYRIDINEDICARBOXIMIDES; ANTICONVULSANT ACTIVITY; NEUROTOXICITY;
D O I：
10.1016/0753-3322(96)82590-X
中图分类号：
R-3 [医学研究方法]; R3 [基础医学];
学科分类号：
1001 ;
摘要：
Two N-(2, 6-dimethylphenyl)pyridinedicarboximides were synthesized and evaluated for anticonvulsant properties and neurotoxicity. These compounds were mainly active against maximal electroshock (MES) induced seizures in animal models. In rats dosed orally, N-(2,6-dimethylphenyl-2,3-pyridinedicarboximide 1 exhibited an anti-MES ED(50) of 54.2 mu mol/kg and a protective ve index (PI =TD50/ED(50) superior to 27.4. In mice dosed intraperitoneally, compound 1 is less active against MES induced seisure (ED(50) = 160.9 mu mol/kg) and more neurotoxic as evidenced by a low protective index (1.93). Comparison with published data on phenytoin reveals that compound 1 is, in rats dosed orally, two-fold more potent than this antiepileptic drug against MES induced seizures.
引用
收藏
页码：75 / 78
页数：4
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