Preparative synthesis and pharmacological activity of Albicar racemate and enantiomers

被引：18

作者：

Anikina, Lada V. ^{[1
]}

Vikharev, Yuri B. ^{[1
]}

Baranov, Vladimir V. ^{[2
]}

Malyshev, Oleg R. ^{[2
]}

Kravchenko, Angelina N. ^{[2
]}

机构：

[1] Russian Acad Sci, Inst Physiol Act Cpds, Chernogolovka 142432, Moscow Region, Russia

[2] Russian Acad Sci, ND Zelinsky Inst Organ Chem, Moscow 119991, Russia

来源：

MENDELEEV COMMUNICATIONS | 2018年 / 28卷 / 03期

基金：

俄罗斯科学基金会;

关键词：

OPEN-FIELD TEST; SELF-ORGANIZATION; MICE; 5-HYDROXYTRYPTOPHAN; GLYCOLURILS; THALIDOMIDE; DRUGS; ACID;

D O I：

10.1016/j.mencom.2018.05.030

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Racemic Albicar (2,6-diethyl-4,8-dimethylglycoluril) has been synthesized and resolved into enantiomers on a preparative scale by chiral HPLC. A comparison of the pharmacological effects of these compounds has been performed for the first time. It has been demonstrated that the (-)-(1S,5S)-enantiomer exerts a stimulating effect on the central nervous system due to activation of the serotonergic system, since it potentiates the effects of 5-hydroxytryptophan (the serotonin precursor), while the antagonist of serotonin receptors blocks its activity; the (+)-(1R,5R)-enantiomer evinces an inhibitory effect.

引用

页码：317 / 319

页数：3

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