Michael J. Waring
Discovery of a series of 2-(pyridinyl) pyrimidines as potent antagonists of GPR40
Waring, Michael J.; Baker, David J.; Bennett, Stuart N.L.; Dossetter, Alexander G.; Fenwick, Mark; Garcia, Rob; Georgsson, Jennie; Groombridge, Sam D.; Loxham, Susan; MacFau, Philip A.; Maskill, Katie G.; Morgan, David; Morrell, Jenny; Pointon, Helen; Robb, Graeme R.; David M. Smith; Stokesa, Stephen; Wilkinson, Gary
Authors
David J. Baker
Stuart N.L. Bennett
Alexander G. Dossetter
Mark Fenwick
Rob Garcia
Jennie Georgsson
Sam D. Groombridge
Susan Loxham
Philip A. MacFau
Katie G. Maskill
David Morgan d.g.a.morgan@keele.ac.uk
Jenny Morrell
Helen Pointon
Graeme R. Robb
David M. Smith
Stephen Stokesa
Gary Wilkinson
Abstract
A series of 2-(pyridinyl)pyrimidines were identified as potent GPR40 antagonists. Despite significant challenges related to improving the combination of potency and lipophilicity within the series, the compounds were optimised to identify a suitable in vivo probe compound, which was confirmed to exhibit pharmacology consistent with GPR40 antagonism.
Citation
Waring, M. J., Baker, D. J., Bennett, S. N., Dossetter, A. G., Fenwick, M., Garcia, R., …Wilkinson, G. (2015). Discovery of a series of 2-(pyridinyl) pyrimidines as potent antagonists of GPR40. MedChemComm, 2015(6), 1024-1029. https://doi.org/10.1039/C5MD00037H
Journal Article Type | Article |
---|---|
Acceptance Date | Apr 1, 2015 |
Publication Date | Apr 8, 2015 |
Journal | MedChemComm |
Print ISSN | 2040-2503 |
Publisher | Royal Society of Chemistry |
Peer Reviewed | Peer Reviewed |
Volume | 2015 |
Issue | 6 |
Pages | 1024-1029 |
DOI | https://doi.org/10.1039/C5MD00037H |
Publisher URL | https://doi.org/10.1039/c5md00037h |
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