New GABA-modulating 1, 2, 4-oxadiazole derivatives and their anticonvulsant activity

…, K Unverferth, C Grunwald, H Hartenhauer…

文献索引：Lankau, Hans-Joachim; Unverferth, Klaus; Grunwald, Christian; Hartenhauer, Helge; Heinecke, Kristina; Bernoester, Katrin; Dost, Rita; Egerland, Ute; Rundfeldt, Chris European Journal of Medicinal Chemistry, 2007 , vol. 42, # 6 p. 873 - 879

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被引用次数: 60

摘要

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 ...