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

被引：74

作者：

Lankau, Hans-Joachim ^{[1
]}

Unverferth, Klaus ^{[1
]}

Grunwald, Christian ^{[1
]}

Hartenhauer, Helge ^{[1
]}

Heinecke, Kristina ^{[1
]}

Bernoester, Katrin ^{[1
]}

Dost, Rita ^{[1
]}

Egerland, Ute ^{[1
]}

Rundfeldt, Chris ^{[1
]}

机构：

[1] Elbion AG, Dept Med Chem, D-01445 Radebuel, Saxony, Germany

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2007年 / 42卷 / 06期

关键词：

1,2,4-oxadiazole derivatives; synthesis; pentylenetetrazole test; maximal electroshock seizure test; anticonvulsant activity;

D O I：

10.1016/j.ejmech.2006.12.022

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

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 1,2,4oxadiazoles 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. (c) 2007 Elsevier Masson SAS. All rights reserved.

引用

页码：873 / 879

页数：7

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