title: Synthesis, characterization and preliminary anticonvulsant evaluation of some 4-alkyl-1,2,4-triazoles.
abstract: Designed and synthesized 4-alkyl-1,2,4-triazole-3-thione derivatives showed significant anticonvulsant activity, determined in the maximal electroshock-induced seizure (MES) test. The chemical structure of all new compounds was confirmed by spectral methods ((1)H NMR, (13)C NMR, IR, MS). A sensitive and selective method was elaborated for the determination of the anticonvulsant compounds levels in mice brain tissue, based on HPLC with diode array detector (DAD). Chromatographic tests showed that lack of anticonvulsant effect of two derivatives (15, 16) with long alkyl chains at N-4 position of the 1,2,4-triazole ring was due to the inability to cross the blood-brain barrier (BBB).
authors.affiliation: Department of Organic Chemistry, Faculty of Pharmacy, Medical University of Lublin, Chodźki 4a, 20-093 Lublin, Poland. tomasz.plech@umlub.pl
authors.forename: Tomasz
authors.initials: T
authors.lastname: Plech
authors.forename: Jarogniew J
authors.initials: JJ
authors.lastname: Luszczki
authors.forename: Monika
authors.initials: M
authors.lastname: Wujec
authors.forename: Jolanta
authors.initials: J
authors.lastname: Flieger
authors.forename: Magdalena
authors.initials: M
authors.lastname: Pizoń
mesh_terms: D000818:Animals; D000927:Anticonvulsants / Q000008:administration & dosage / Q000138:chemical synthesis / Q000494:pharmacology*; D004597:Electroshock / Q000009:adverse effects; D008297:Male; D051379:Mice; D015394:Molecular Structure; D012640:Seizures / Q000188:drug therapy* / Q000517:prevention & control; D014230:Triazoles / Q000008:administration & dosage / Q000138:chemical synthesis / Q000494:pharmacology*
chemical_list: D000927:Anticonvulsants; D014230:Triazoles; C045575:1,2,4-triazole