title: Studies on the anticonvulsant activity and influence on GABA-ergic neurotransmission of 1,2,4-triazole-3-thione- based compounds.
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.
authors.affiliation: Department of Organic Chemistry, Medical University of Lublin, Chodźki 4a, Lublin 20-093, Poland. tomasz.plech@umlub.pl.
authors.forename: Tomasz
authors.initials: T
authors.lastname: Plech
authors.affiliation: Department of Organic Chemistry, Medical University of Lublin, Chodźki 4a, Lublin 20-093, Poland. baska_k@o2.pl.
authors.forename: Barbara
authors.initials: B
authors.lastname: Kaproń
authors.affiliation: Department of Pathophysiology, Medical University of Lublin, Jaczewskiego 8, Lublin 20-090, Poland. jarogniew.luszczki@gmail.com.
authors.forename: Jarogniew J
authors.initials: JJ
authors.lastname: Luszczki
authors.affiliation: Department of Organic Chemistry, Medical University of Lublin, Chodźki 4a, Lublin 20-093, Poland. monika.wujec@umlub.pl.
authors.forename: Monika
authors.initials: M
authors.lastname: Wujec
authors.affiliation: Department of Organic Chemistry, Medical University of Lublin, Chodźki 4a, Lublin 20-093, Poland. agata.siwek@umlub.pl.
authors.forename: Agata
authors.initials: A
authors.lastname: Paneth
authors.affiliation: Department of Pharmacobiology, Jagiellonian University Medical College, Medyczna 9, Kraków 30-688, Poland. asiwku@wp.pl.
authors.forename: Agata
authors.initials: A
authors.lastname: Siwek
authors.affiliation: Department of Pharmaceutical Chemistry, Jagiellonian University Medical College, Medyczna 9, Kraków 30-688, Poland. mkolacz@tlen.pl.
authors.forename: Marcin
authors.initials: M
authors.lastname: Kołaczkowski
authors.affiliation: Department of Pharmacobiology, Jagiellonian University Medical College, Medyczna 9, Kraków 30-688, Poland. mfzolnie@cyf-kr.edu.pl.
authors.forename: Maria
authors.initials: M
authors.lastname: Zołnierek
authors.affiliation: Department of Pharmacobiology, Jagiellonian University Medical College, Medyczna 9, Kraków 30-688, Poland. nowak@if-pan.krakow.pl.
authors.forename: Gabriel
authors.initials: G
authors.lastname: Nowak
mesh_terms: D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis / Q000494:pharmacology*; D004195:Disease Models, Animal; D018682:GABA Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D008297:Male; D051379:Mice; D012640:Seizures / Q000188:drug therapy; D009435:Synaptic Transmission / Q000187:drug effects*; D018675:Toxicity Tests; D014230:Triazoles / Q000138:chemical synthesis / Q000494:pharmacology*
chemical_list: D000927:Anticonvulsants; D018682:GABA Agents; D014230:Triazoles
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