کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1393315 1501203 2009 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis and anticonvulsant activity of some substituted 1,2,4-thiadiazoles
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Synthesis and anticonvulsant activity of some substituted 1,2,4-thiadiazoles
چکیده انگلیسی

A series of new substituted 1,2,4-thiadiazoles were synthesized by appropriate route and screened for anticonvulsant, neurotoxic and sedative-hypnotic activity. The structures of the synthesized compounds were confirmed by IR spectroscopy, 13C NMR and elemental (nitrogen and sulphur) analysis. After i.p. injection of the compounds to mice or rate at doses of 30, 100, and 300 mg/kg, body weights were examined in the maximal electroshock-induced seizures (MES) and subcutaneous pentylenetetrazole (scPTZ)-induced seizure models after 0.5 and 4 h. Rotorod method and phenobarbitone-induced hypnosis potentiation study were employed to examine neurotoxicity and sedative-hypnotic activity, respectively. All the compounds except 4g showed protection against MES screen after 0.5 h. Compounds 3a–c, 4a–c were active at 100 mg/kg dose i.p., whereas remaining compounds showed activity at 300 mg/kg. All 14 compounds except 3 g showed neurotoxicity at 100 and 300 mg/kg after 0.5 h. Compounds 3b and 4b showed NT after 4 h. Two compounds 3b and 4g showed significant (p < 0.05) percentage increase in sleeping time i.e. 67% and 59%, respectively. It may be concluded that the synthesized compounds were potent against MES-induced seizures than ScPTZ induced and showed low potency as sedative-hypnotic agent which is advantageous.

A series of new substituted 1,2,4-thiadiazole have been synthesized and evaluated for anticonvulsant and neurotoxicity by maximal electroshock-induced seizures (MESs) and subcutaneous pentylenetetrazole (scPTZ)-induced seizure models in mice. Synthesized compounds were potent against MES-induced seizures than ScPTZ induced.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Medicinal Chemistry - Volume 44, Issue 3, March 2009, Pages 1100–1105
نویسندگان
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