Show simple item record

dc.contributor.authorKaris, Daviden_US
dc.contributor.authorLoughlin, Wendyen_US
dc.contributor.authorJenkins, Ianen_US
dc.contributor.authorHealy, Peteren_US
dc.date.accessioned2017-04-24T09:20:38Z
dc.date.available2017-04-24T09:20:38Z
dc.date.issued2009en_US
dc.date.modified2010-06-25T07:01:41Z
dc.identifier.issn09680896en_US
dc.identifier.doi10.1016/j.bmc.2009.04.049en_AU
dc.identifier.urihttp://hdl.handle.net/10072/29546
dc.description.abstractGlycogen 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 卩. 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.en_US
dc.description.peerreviewedYesen_US
dc.description.publicationstatusYesen_AU
dc.languageEnglishen_US
dc.language.isoen_AU
dc.publisherPergamonen_US
dc.publisher.placeUnited Kingdomen_US
dc.publisher.urihttp://www.sciencedirect.com/science/journal/09680896en_AU
dc.relation.ispartofstudentpublicationNen_AU
dc.relation.ispartofpagefrom4724en_US
dc.relation.ispartofpageto4733en_US
dc.relation.ispartofjournalBioorganic & Medicinal Chemistryen_US
dc.relation.ispartofvolume17en_US
dc.rights.retentionYen_AU
dc.subject.fieldofresearchBiologically Active Moleculesen_US
dc.subject.fieldofresearchcode030401en_US
dc.titleGlycogen phosphorylase inhibitory effects of 2-oxo-1,2-dihydropyridin-3-yl amide derivativesen_US
dc.typeJournal articleen_US
dc.type.descriptionC1 - Peer Reviewed (HERDC)en_US
dc.type.codeC - Journal Articlesen_US
gro.facultyGriffith Sciences, Griffith Institute for Drug Discoveryen_US
gro.date.issued2009
gro.hasfulltextNo Full Text


Files in this item

FilesSizeFormatView

There are no files associated with this item.

This item appears in the following Collection(s)

  • Journal articles
    Contains articles published by Griffith authors in scholarly journals.

Show simple item record