Synthesis and anticonvulsant activity of new phenytoin derivatives

被引：53
|
作者：
Botros, S. [1 ]
Khalil, Nadia A. [1 ]
Naguib, Bassem H. [1 ]
El-Dash, Yara [1 ]
机构：
[1] Cairo Univ, Fac Pharm, Dept Organ Pharmaceut Chem, Cairo, Egypt
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2013年 / 60卷
关键词：
Phenytoin; Oxadiazole; Thiadiazole; Triazole; Anticonvulsant activity; ANTIMICROBIAL ACTIVITIES; ANIMAL-MODELS; EPILEPSY; DRUGS; PENTYLENETETRAZOLE; THIOSEMICARBAZIDES; 1,2,4-TRIAZOLES; AGENTS; MICE;
D O I：
10.1016/j.ejmech.2012.11.025
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Hybrids between phenytoin and thiosemicarbazide, 1,3,4-oxadiazole, 1,3,4-thiadiazole or 1,2,4-triazole were synthesized and tested for anticonvulsant activity. Preliminary anticonvulsant screening was performed using standard maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) screens in mice. The neurotoxicity was determined applying the rotarod test. Among these compounds, 4 and 5d showed the highest protection (80%) in the scPTZ test at a dose of 100 mg/kg, whereas the compound 5b displayed promising anticonvulsant effect in the MES model. (C) 2012 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码：57 / 63
页数：7
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