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

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. MacFaul; Katie G. Maskill; David Morgan; Jenny Morrell; Helen Pointon; Graeme R. Robb; David M. Smith; Stephen Stokes; Gary Wilkinson

doi:10.1039/C5MD00037H

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

Michael J. Waring,*^a David J. Baker,^a Stuart N. L. Bennett,^a Alexander G. Dossetter,^a Mark Fenwick,^a Rob Garcia,^a Jennie Georgsson,^a Sam D. Groombridge,^a Susan Loxham,^a Philip A. MacFaul,^a Katie G. Maskill,^a David Morgan,^a Jenny Morrell,^a Helen Pointon,^a Graeme R. Robb,^a David M. Smith,^a Stephen Stokes^a and Gary Wilkinson

^a

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^a AstraZeneca, Mereside, Alderley Park, Macclesfield, Cheshire, UK
E-mail: mike.j.waring@astrazeenca.com
Tel: +44 (0) 1625 230942

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.

MedChemComm

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

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

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