Phenytoin-based bivalent ligands: Design, synthesis and anticonvulsant activity

被引：3
作者：
Botros, Samir [1 ]
Khalil, Nadia A. [1 ]
Naguib, Bassem H. [1 ]
El-Dash, Yara [1 ]
机构：
[1] Cairo Univ, Dept Organ Pharmaceut Chem, Fac Pharm, Cairo 11562, Egypt
来源：
ARCHIVES OF PHARMACAL RESEARCH | 2012年 / 35卷 / 12期
关键词：
Phenytoin; Bivalent ligands; Anticonvulsant activity; ANTIEPILEPTIC DRUGS; MOLECULAR-PROPERTIES; ANIMAL-MODELS; PENTYLENETETRAZOLE; PERMEABILITY; DERIVATIVES; PREDICTION; ANALOGS;
D O I：
10.1007/s12272-012-1207-3
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Synthesis, characterization and anticonvulsant properties of new bivalent ligands derived from phenytoin were described. Initial anticonvulsant screening was performed using maximal electroshock (MES) and pentylenetetrazole (PTZ) screens in mice. The neurotoxicity for compounds that showed significant anticonvulsant activity was determined applying the rotorod test. Most of the test compounds were found to be effective in at least one seizure model in a dose of 100 mg/kg. Compound 5e exhibited marked anticonvulsant activity in both MES and PTZ screens. The computer-aided prediction of biological activity was carried out.
引用
收藏
页码：2105 / 2116
页数：12
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