Department of Organic Chemistry, Faculty of Pharmacy, Medical University of Lublin, Chodźki 4a, 20-093 Lublin, Poland.
Eur J Med Chem. 2013 Feb;60:208-15. doi: 10.1016/j.ejmech.2012.11.026. Epub 2012 Nov 23.
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).
设计并合成的 4-烷基-1,2,4-三唑-3-硫酮衍生物在最大电休克诱导的惊厥（MES）试验中表现出显著的抗惊厥活性。所有新化合物的化学结构均通过光谱方法（1H NMR、13C NMR、IR、MS）确认。基于 HPLC 与二极管阵列检测器（DAD），建立了一种用于测定小鼠脑组织中抗惊厥化合物水平的灵敏、选择性方法。色谱试验表明，由于无法穿过血脑屏障（BBB），N-4 位具有长烷基链的两个衍生物（15、16）没有抗惊厥作用。
