Glycogen phosphorylase inhibitory effects of 2-oxo-1,2-dihydropyridin-3-yl amide derivatives

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Title Glycogen phosphorylase inhibitory effects of 2-oxo-1,2-dihydropyridin-3-yl amide derivatives
Author Karis, David; Loughlin, Wendy Anne; Jenkins, Ian Douglas; Healy, Peter Conrad
Journal Name Bioorganic & Medicinal Chemistry
Year Published 2009
Place of publication United Kingdom
Publisher Pergamon
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 (IC50 = 6.3 μM). 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.
Peer Reviewed Yes
Published Yes
Publisher URI
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Volume 17
Page from 4724
Page to 4733
ISSN 0968-0896
Date Accessioned 2009-09-22
Date Available 2010-06-25T07:01:41Z
Language en_AU
Faculty Faculty of Science, Environment, Engineering and Technology
Subject Biologically Active Molecules
Publication Type Journal Articles (Refereed Article)
Publication Type Code c1

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