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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

Discovery of a series of 2-(pyridinyl) pyrimidines as potent antagonists of GPR40 Thumbnail


Authors

Michael J. Waring

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

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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