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Molecules 2014, 19(8), 11279-11299; https://doi.org/10.3390/molecules190811279

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

1
Department of Organic Chemistry, Medical University of Lublin, Chodźki 4a, Lublin 20-093, Poland
2
Department of Pathophysiology, Medical University of Lublin, Jaczewskiego 8, Lublin 20-090, Poland
3
Isobolographic Analysis Laboratory, Institute of Rural Health, Jaczewskiego 2, Lublin 20-950, Poland
4
Department of Pharmacobiology, Jagiellonian University Medical College, Medyczna 9, Kraków 30-688, Poland
5
Department of Pharmaceutical Chemistry, Jagiellonian University Medical College, Medyczna 9, Kraków 30-688, Poland
*
Author to whom correspondence should be addressed.
Received: 3 July 2014 / Revised: 22 July 2014 / Accepted: 23 July 2014 / Published: 31 July 2014
(This article belongs to the Section Medicinal Chemistry)
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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. View Full-Text
Keywords: 30-688 s-triazoles; Mannich bases; maximal electroshock-induced seizure (MES) test; blood-brain barrier (BBB); radioligand binding assay 30-688 s-triazoles; Mannich bases; maximal electroshock-induced seizure (MES) test; blood-brain barrier (BBB); radioligand binding assay
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This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).
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Plech, T.; Kaproń, B.; Łuszczki, J.J.; Wujec, M.; Paneth, A.; Siwek, A.; Kołaczkowski, M.; Żołnierek, M.; Nowak, G. Studies on the Anticonvulsant Activity and Influence on GABA-ergic Neurotransmission of 1,2,4-Triazole-3-thione- Based Compounds. Molecules 2014, 19, 11279-11299.

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