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  • Title: Glycogen phosphorylase inhibitory effects of 2-oxo-1,2-dihydropyridin-3-yl amide derivatives.
    Author: Karis ND, Loughlin WA, Jenkins ID, Healy PC.
    Journal: Bioorg Med Chem; 2009 Jul 01; 17(13):4724-33. PubMed ID: 19443226.
    Abstract:
    Glycogen phosphorylase (GP) plays a crucial role in the conversion of glycogen to glucose-1-phosphate (and in turn glucose) and is a promising target for therapeutic intervention in diabetes. In this study we synthesized new derivatives of 2-oxo-1,2-dihydropyridin-3-yl amides using a facile aminolysis reaction, in which different alkyl and aryl esters and amides are substituted at N-1 and C-3 of the heterocyclic ring. The in vitro inhibitory activity of compounds against glycogen phosphorylase was evaluated. From this series the most potent compound exhibits good GPa inhibition (IC(50)=6.3 microM). A preliminary study of these compounds showed that anti-GP activity was decreased by the incorporation of a C3-N carbonyl group and favored by increased lipophilicity.
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