Synthesis, characterization and preliminary anticonvulsant evaluation of some 4-alkyl-1,2,4-triazoles

被引：82

作者：

Plech, Tomasz ^{[1
]}

Luszczki, Jarogniew J. ^{[2
,3
]}

Wujec, Monika ^{[1
]}

Flieger, Jolanta ^{[4
]}

Pizon, Magdalena ^{[4
]}

机构：

[1] Med Univ Lublin, Fac Pharm, Dept Organ Chem, PL-20093 Lublin, Poland

[2] Med Univ Lublin, Dept Pathophysiol, PL-20090 Lublin, Poland

[3] Inst Rural Hlth, Isobolog Anal Lab, PL-20950 Lublin, Poland

[4] Med Univ Lublin, Dept Analyt Chem, PL-20093 Lublin, Poland

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2013年 / 60卷

关键词：

s-Triazole; Blood-brain barrier; MES test; Chimney test; HPLC/DAD; CLASSICAL ANTIEPILEPTIC DRUGS; INDUCED SEIZURE MODEL; VALPROATE; MOUSE; PHARMACOKINETICS; MECHANISMS; EPILEPSY; ACID; MICE;

D O I：

10.1016/j.ejmech.2012.11.026

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 (H-1 NMR, C-13 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). (C) 2012 Elsevier Masson SAS. All rights reserved.

引用

页码：208 / 215

页数：8

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