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New GABA-modulating 1,2,4-oxadiazole derivatives and their anticonvulsant activity
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Abstract
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 ED(50) of 25.5mg/kg
and in the MES model in rats with an oral ED(50) of 14.6mg/kg. Neurotoxicity (rotarod)
was observed with an ED(50) of 335mg/kg. We found several oxadiazoles that acted as
selective GABA potentiating compounds with no interaction to the benzodiazepine binding
site.