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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...
Autores principales: | , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2014
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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. |
format | Online Article Text |
id | pubmed-6271529 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2014 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
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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