dc.contributor.author | Loughlin, Wendy A | |
dc.contributor.author | Jenkins, Ian D | |
dc.contributor.author | Karis, N David | |
dc.contributor.author | Schweiker, Stephanie S | |
dc.contributor.author | Healy, Peter C | |
dc.date.accessioned | 2019-02-28T05:30:47Z | |
dc.date.available | 2019-02-28T05:30:47Z | |
dc.date.issued | 2016 | |
dc.identifier.issn | 0223-5234 | |
dc.identifier.doi | 10.1016/j.ejmech.2016.01.031 | |
dc.identifier.uri | http://hdl.handle.net/10072/99962 | |
dc.description.abstract | Glycogen 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.peerreviewed | Yes | |
dc.language | English | |
dc.language.iso | eng | |
dc.publisher | Editions Elsevier | |
dc.relation.ispartofpagefrom | 1 | |
dc.relation.ispartofpageto | 14 | |
dc.relation.ispartofjournal | European Journal of Medicinal Chemistry | |
dc.relation.ispartofvolume | 111 | |
dc.subject.fieldofresearch | Organic chemical synthesis | |
dc.subject.fieldofresearch | Biologically active molecules | |
dc.subject.fieldofresearchcode | 340503 | |
dc.subject.fieldofresearchcode | 340401 | |
dc.title | 2-Oxo-1,2-dihydropyridinyl-3-yl amide-based GPa inhibitors: Design, synthesis and structure-activity relationship study | |
dc.type | Journal article | |
dc.type.description | C1 - Articles | |
dc.type.code | C - Journal Articles | |
gro.faculty | Griffith Sciences, School of Natural Sciences | |
gro.hasfulltext | No Full Text | |
gro.griffith.author | Jenkins, Ian D. | |
gro.griffith.author | Healy, Peter C. | |
gro.griffith.author | Loughlin, Wendy A. | |