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dc.contributor.authorLoughlin, Wendy A
dc.contributor.authorJenkins, Ian D
dc.contributor.authorKaris, N David
dc.contributor.authorSchweiker, Stephanie S
dc.contributor.authorHealy, Peter C
dc.date.accessioned2019-02-28T05:30:47Z
dc.date.available2019-02-28T05:30:47Z
dc.date.issued2016
dc.identifier.issn0223-5234
dc.identifier.doi10.1016/j.ejmech.2016.01.031
dc.identifier.urihttp://hdl.handle.net/10072/99962
dc.description.abstractGlycogen phosphorylase (GP), which plays a crucial role in the conversion of glycogen to glucose-1-phosphate, is a target for therapeutic intervention in diabetes. In this study, we report the design and synthesis of 29 new derivatives of 2-oxo-1,2-dihydro pyridin-3-yl amides, as potential inhibitors of GP. The hit rate (45%) was high with 13 compounds inhibiting GPa (between 33% at 4.40 mM and an IC50 of 1.92 μM). Two lead compounds were identified as compounds exhibiting good GPa inhibition (IC50 = 2.1 and 1.92 μM). SAR analysis of these compounds revealed sensitivity of GPa to the length of the 2-oxo-1,2-dihydro pyridin-3-yl amide derivative and a preference for inclusion of a 3,4-dichlorobenzyl moiety.
dc.description.peerreviewedYes
dc.languageEnglish
dc.language.isoeng
dc.publisherEditions Elsevier
dc.relation.ispartofpagefrom1
dc.relation.ispartofpageto14
dc.relation.ispartofjournalEuropean Journal of Medicinal Chemistry
dc.relation.ispartofvolume111
dc.subject.fieldofresearchOrganic chemical synthesis
dc.subject.fieldofresearchBiologically active molecules
dc.subject.fieldofresearchcode340503
dc.subject.fieldofresearchcode340401
dc.title2-Oxo-1,2-dihydropyridinyl-3-yl amide-based GPa inhibitors: Design, synthesis and structure-activity relationship study
dc.typeJournal article
dc.type.descriptionC1 - Articles
dc.type.codeC - Journal Articles
gro.facultyGriffith Sciences, School of Natural Sciences
gro.hasfulltextNo Full Text
gro.griffith.authorJenkins, Ian D.
gro.griffith.authorHealy, Peter C.
gro.griffith.authorLoughlin, Wendy A.


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