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Updated: Jul 16, 2026

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
Published on: August 16, 2018
New GABA-modulating 1,2,4-oxadiazole derivatives and their anticonvulsant activity
Hans-Joachim Lankau1, Klaus Unverferth, Christian Grunwald
1Department of Medicinal Chemistry, elbion AG, Meissner Strasse 191, D-01445 Radebeul, Saxony, Germany. hans-joachim.lankau@elbion.de
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.
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