Fructose-fused γ-butyrolactones and lactams, synthesis and biological evaluation as GABA receptor ligands

被引:22
作者
Araujo, Ana C. [2 ,3 ]
Nicotra, Francesco [1 ]
Costa, Barbara [1 ]
Giagnoni, Gabriella [1 ]
Cipolla, Laura [1 ]
机构
[1] Univ Milano Bicocca, Dept Biosci & Biotechnol, I-20126 Milan, Italy
[2] Univ Lisbon, Dept Quim & Bioquim, P-1749016 Lisbon, Portugal
[3] CQB, P-1749016 Lisbon, Portugal
关键词
C-glycosides; fructose; gamma-butyrolactones; gamma-butyrolactams; GABA receptors;
D O I
10.1016/j.carres.2008.03.013
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
We describe the synthesis of sugar-fused beta-disubstituted gamma-butyrolactones, gamma-butyrolactams and a lipophilic beta-disubstituted GABA analogue as potential GABA receptor ligands, where the pharmacophore is engineered into the carbohydrate scaffold in the form of a C-fructoside. The products were characterized for receptor binding studies of GABA(A) receptors. (c) 2008 Elsevier Ltd. All rights reserved.
引用
收藏
页码:1840 / 1848
页数:9
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