کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1359083 981380 2010 9 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Design, synthesis, and anticonvulsant activity of new N-Mannich bases derived from spirosuccinimides and spirohydantoins
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Design, synthesis, and anticonvulsant activity of new N-Mannich bases derived from spirosuccinimides and spirohydantoins
چکیده انگلیسی

The synthesis and anticonvulsant properties of new N-Mannich bases of [7,8-f]benzo-2-aza-spiro[4.5]decane-1,3-diones (5a–h) and [7,8-f]benzo-1,3-diaza-spiro[4.5]decane-2,4-diones (7a–h) were described. Initial anticonvulsant screening was performed using intraperitoneal (ip) maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) seizures tests. The neurotoxicity was determined applying the rotarod test. The majority of compounds were effective in the MES or/and scPTZ screen. The quantitative studies showed that several molecules were more potent than phenytoin, used as reference drug. Selected derivatives were screened in the 6-Hz test and also assessed for potential activity against nerve agents using the Pilocarpine Induced Status Prevention model. To explain the possible mechanism of anticonvulsant action, for chosen active derivatives, their influence on voltage-dependent Na+ channel were tested in vitro.

Majority of compounds synthesized showed high activity in the maximal electroshock test (MES). To explain the possible mechanism of anticonvulsant action, for chosen active derivatives, their influence on voltage-dependent Na+ channel were tested in vitro.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 18, Issue 16, 15 August 2010, Pages 6134–6142
نویسندگان
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