کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1395579 | 1501223 | 2007 | 7 صفحه PDF | دانلود رایگان |
A series of 3- and 5-aryl-1,2,4-oxadiazole derivatives were prepared and tested for anticonvulsant activity in a variety of models. These 1,2,4-oxadiazoles exhibit considerable activity in both pentylenetetrazole (PTZ) and maximal electroshock seizure (MES) models. Compound 10 was protective in the PTZ model in rats with an oral ED50 of 25.5 mg/kg and in the MES model in rats with an oral ED50 of 14.6 mg/kg. Neurotoxicity (rotarod) was observed with an ED50 of 335 mg/kg. We found several oxadiazoles that acted as selective GABA potentiating compounds with no interaction to the benzodiazepine binding site.
New 3- and 5-aryl-1,2,4-oxadiazole derivatives are described that act as selective GABA potentiating compounds with no interaction to the benzodiazepine binding site and compound 10 was found to be most effective.Figure optionsDownload as PowerPoint slide
Journal: European Journal of Medicinal Chemistry - Volume 42, Issue 6, June 2007, Pages 873–879