کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1399260 1501156 2013 7 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis and anticonvulsant activity of new phenytoin derivatives
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Synthesis and anticonvulsant activity of new phenytoin derivatives
چکیده انگلیسی

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.

Hybrid approach was used to design and synthesize hybrids between phenytoin and thiosemicarbazide, 1,3,4-oxadiazole, 1,3,4-thiadiazole or 1,2,4-triazole pharmacophores to examine their anticonvulsant activity using MES and scPTZ screens in mice.Figure optionsDownload as PowerPoint slideHighlights
► Synthesis of phenytoin derivatives.
► Anticonvulsant activity of all new synthesized compounds was determined.
► Neurotoxicity of the most active compounds was estimated.
► Compounds 4, 5b and 5d demonstrated marked anticonvulsant effect.
► Elemental analysis and spectroscopic characterization of all new compounds.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Medicinal Chemistry - Volume 60, February 2013, Pages 57–63
نویسندگان
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