具有抗缺氧和抗惊厥活性的新型4-芳基氨基哌啶类化合物。
New 4-arylaminopiperidines with antihypoxic and anticonvulsive activity.
作者信息
Domány G, Barta-Szalai G, Pálosi E, Szabó S, Schön I
机构信息
Chemical Works of Gedeon Richter Ltd., Budapest, Hungary.
出版信息
Arzneimittelforschung. 1994 Sep;44(9):989-91.
PMID:7986252
Abstract
Several new bioanalogues of (+/-)-N-methyl-N-(1-[3-(4-fluorophenoxy)-2-hydroxy-propyl]piperidin++ +-4-yl) benzothiazol-2-amine (1, sabeluzole, CAS 104383-17-7) were prepared by reacting 1,2-epoxy-3-aryloxypropanes with 4-arylaminopiperidines. Some of these derivatives showed enhanced activity in the potassium cyanide hypoxia test and in the pentetrazol convulsion test in mice compared to 1.
摘要
通过使1,2 - 环氧 - 3 - 芳氧基丙烷与4 - 芳基氨基哌啶反应，制备了几种(±)-N - 甲基 - N -(1 - [3 - (4 - 氟苯氧基)-2 - 羟基丙基]哌啶 - 4 - 基)苯并噻唑 - 2 - 胺（1，沙贝鲁唑，CAS 104383 - 17 - 7）的新型生物类似物。与1相比，其中一些衍生物在小鼠的氰化钾缺氧试验和戊四氮惊厥试验中显示出增强的活性。
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