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新型γ-羟基丁酸衍生物的合成及初步药理学评估

Synthesis and preliminary pharmacological assessment of novel gamma-hydroxybutyric acid derivatives.

作者信息

Malec D, Modzelewski J, Malawska B, Gorczyca M

机构信息

Department of Pharmacodynamics, Medical Academy, Lublin, Poland.

出版信息

Pol J Pharmacol Pharm. 1990 Sep-Oct;42(5):491-500.

PMID:2098756
Abstract

Synthesis and properties of new N-substituted amides of alpha-(1,1-ethylenedioxy)-ethyl-gamma-hydroxybutyric acid are described. The compounds were obtained by aminolysis of 3-(1,1-ethylenedioxy)-ethyltetra-hydrofuran-2-on with primary alkylarylamines. Preliminary pharmacological assessment revealed that the compounds exert weaker influence on the central nervous system than the reference gamma-hydroxybutyric acid. Three of the novel compounds offered some protection against pentetrazole-induced tonic seizures in mice.

摘要

描述了新型α-(1,1-乙二氧基)-乙基-γ-羟基丁酸的N-取代酰胺的合成及其性质。这些化合物是通过3-(1,1-乙二氧基)-乙基四氢呋喃-2-酮与伯烷基芳胺进行氨解反应制得的。初步药理学评估表明,这些化合物对中枢神经系统的影响比参比γ-羟基丁酸弱。其中三种新型化合物对小鼠戊四氮诱导的强直性惊厥有一定的保护作用。

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