Studies on the anticonvulsant activity and influence on GABA-ergic neurotransmission of 1,2,4-triazole-3-thione- based compounds

1,2,4-三唑-3-硫酮类化合物的抗惊厥活性及对GABA能神经传递的影响研究

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作者:Tomasz Plech, Barbara Kaproń, Jarogniew J Luszczki, Monika Wujec, Agata Paneth, Agata Siwek, Marcin Kołaczkowski, Maria Zołnierek, Gabriel Nowak

Abstract

The anticonvulsant activity of several 1,2,4-triazole-3-thione derivatives on mouse maximal electroshock-induced seizures was tested in this study. Characteristic features of all active compounds were rapid onset of action and long lasting effect. Structure-activity observations showed that the probability of obtaining compounds exerting anticonvulsant activity was much higher when at least one of the phenyl rings attached to 1,2,4-triazole nucleus had a substituent at the para position. The obtained results, moreover, permit us to conclude that despite the structural similarity of loreclezole (second-generation anticonvulsant drug) and the titled compounds, their anticonvulsant activity is achieved via completely different molecular mechanisms.

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