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一些新型1,1-双(4-取代-1,2,4-三唑啉-5-硫酮-3-基)-2-甲基丁烷的合成及其抗惊厥活性

Synthesis and anticonvulsant activity of some new 1,1-bis(4-substituted 1,2,4-triazoline-5-thione-3-yl)-2-methylbutanes.

作者信息

Ergenç N, Ulusoy N, Ekinci A C

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Istanbul, Turkey.

出版信息

Farmaco. 1995 Mar;50(3):189-92.

PMID:7755867
Abstract

Several 1,1-bis(4-alkyl/aryl-1,2,4-triazoline-5-thione-3-yl)-2- methylbutane derivatives 13-21 were obtained from the cyclization of mono(1-methylpropyl)malonylbis(4-alkyl/aryl)thiosemicarbazides 2-12 in the presence of sodium hydroxide. Their chemical structures were proven by spectral data (UV, IR, 1H-NMR, MS) and elemental analysis. The anticonvulsant activity of the title compounds were determined against pentylenetetrazole induced seizures. Six of the tested compounds showed anticonvulsant activity (10 to 20% protection).

摘要

通过在氢氧化钠存在下使单(1-甲基丙基)丙二酰双(4-烷基/芳基)硫代氨基脲2-12环化,得到了几种1,1-双(4-烷基/芳基-1,2,4-三唑啉-5-硫酮-3-基)-2-甲基丁烷衍生物13-21。它们的化学结构通过光谱数据(紫外、红外、1H-核磁共振、质谱)和元素分析得以证实。测定了标题化合物对戊四氮诱导惊厥的抗惊厥活性。六种受试化合物显示出抗惊厥活性(保护率为10%至20%)。

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