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Studies on the Anticonvulsant Activity and Influence on GABA-ergic Neurotransmission of 1,2,4-Triazole-3-thione-Based Compounds

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 prob...

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Autores principales: Plech, Tomasz, Kaproń, Barbara, Łuszczki, Jarogniew J., Wujec, Monika, Paneth, Agata, Siwek, Agata, Kołaczkowski, Marcin, Żołnierek, Maria, Nowak, Gabriel
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2014
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6271529/
https://www.ncbi.nlm.nih.gov/pubmed/25090118
http://dx.doi.org/10.3390/molecules190811279
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author Plech, Tomasz
Kaproń, Barbara
Łuszczki, Jarogniew J.
Wujec, Monika
Paneth, Agata
Siwek, Agata
Kołaczkowski, Marcin
Żołnierek, Maria
Nowak, Gabriel
author_facet Plech, Tomasz
Kaproń, Barbara
Łuszczki, Jarogniew J.
Wujec, Monika
Paneth, Agata
Siwek, Agata
Kołaczkowski, Marcin
Żołnierek, Maria
Nowak, Gabriel
author_sort Plech, Tomasz
collection PubMed
description 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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spelling pubmed-62715292018-12-27 Studies on the Anticonvulsant Activity and Influence on GABA-ergic Neurotransmission of 1,2,4-Triazole-3-thione-Based Compounds Plech, Tomasz Kaproń, Barbara Łuszczki, Jarogniew J. Wujec, Monika Paneth, Agata Siwek, Agata Kołaczkowski, Marcin Żołnierek, Maria Nowak, Gabriel Molecules Article 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. MDPI 2014-07-31 /pmc/articles/PMC6271529/ /pubmed/25090118 http://dx.doi.org/10.3390/molecules190811279 Text en © 2014 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
Plech, Tomasz
Kaproń, Barbara
Łuszczki, Jarogniew J.
Wujec, Monika
Paneth, Agata
Siwek, Agata
Kołaczkowski, Marcin
Żołnierek, Maria
Nowak, Gabriel
Studies on the Anticonvulsant Activity and Influence on GABA-ergic Neurotransmission of 1,2,4-Triazole-3-thione-Based Compounds
title Studies on the Anticonvulsant Activity and Influence on GABA-ergic Neurotransmission of 1,2,4-Triazole-3-thione-Based Compounds
title_full Studies on the Anticonvulsant Activity and Influence on GABA-ergic Neurotransmission of 1,2,4-Triazole-3-thione-Based Compounds
title_fullStr Studies on the Anticonvulsant Activity and Influence on GABA-ergic Neurotransmission of 1,2,4-Triazole-3-thione-Based Compounds
title_full_unstemmed Studies on the Anticonvulsant Activity and Influence on GABA-ergic Neurotransmission of 1,2,4-Triazole-3-thione-Based Compounds
title_short Studies on the Anticonvulsant Activity and Influence on GABA-ergic Neurotransmission of 1,2,4-Triazole-3-thione-Based Compounds
title_sort studies on the anticonvulsant activity and influence on gaba-ergic neurotransmission of 1,2,4-triazole-3-thione-based compounds
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6271529/
https://www.ncbi.nlm.nih.gov/pubmed/25090118
http://dx.doi.org/10.3390/molecules190811279
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