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  • Title: C-Glucosylated malonitrile as a key intermediate towards carbohydrate-based glycogen phosphorylase inhibitors.
    Author: Feuillastre S, Chajistamatiou AS, Potamitis C, Zervou M, Zoumpoulakis P, Chrysina ED, Praly JP, Vidal S.
    Journal: Bioorg Med Chem; 2012 Sep 15; 20(18):5592-9. PubMed ID: 22910227.
    Abstract:
    Glycogen utilization involves glycogen phosphorylase, an enzyme which appears to be a potential target for the regulation of glycaemia, as the liver isoform is a major player for hepatic glucose output. A single C-glucosylated malonitrile allowed for the synthesis of three glucose-based derivatives namely bis-oxadiazoles, bis-amides and a C-glucosylated tetrahydropyrimidin-2-one. When evaluated as glycogen phosphorylase inhibitors, two of the synthesized compounds displayed inhibition in the sub-millimolar range. In silico studies revealed that only one out of the bis-amides obtained and the C-glucosylated tetrahydropyrimidin-2-one may bind at the catalytic site.
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