Structure-Activity Relationship and Crystallographic Studies on 4-Hydroxypyrimidine HIF Prolyl Hydroxylase Domain Inhibitors.

Autor:	Holt-Martyn JP; Department of Chemistry, University of Oxford Chemistry Research Laboratory, 12 Mansfield Road, Oxford, OX1 3TA, UK., Chowdhury R; Department of Chemistry, University of Oxford Chemistry Research Laboratory, 12 Mansfield Road, Oxford, OX1 3TA, UK., Tumber A; Department of Chemistry, University of Oxford Chemistry Research Laboratory, 12 Mansfield Road, Oxford, OX1 3TA, UK., Yeh TL; Department of Chemistry, University of Oxford Chemistry Research Laboratory, 12 Mansfield Road, Oxford, OX1 3TA, UK., Abboud MI; Department of Chemistry, University of Oxford Chemistry Research Laboratory, 12 Mansfield Road, Oxford, OX1 3TA, UK., Lippl K; Department of Chemistry, University of Oxford Chemistry Research Laboratory, 12 Mansfield Road, Oxford, OX1 3TA, UK., Lohans CT; Department of Chemistry, University of Oxford Chemistry Research Laboratory, 12 Mansfield Road, Oxford, OX1 3TA, UK., Langley GW; Department of Chemistry, University of Oxford Chemistry Research Laboratory, 12 Mansfield Road, Oxford, OX1 3TA, UK., Figg W Jr; Department of Chemistry, University of Oxford Chemistry Research Laboratory, 12 Mansfield Road, Oxford, OX1 3TA, UK., McDonough MA; Department of Chemistry, University of Oxford Chemistry Research Laboratory, 12 Mansfield Road, Oxford, OX1 3TA, UK., Pugh CW; NDM Research Building, University of Oxford, Oxford, OX3 7FZ, UK., Ratcliffe PJ; NDM Research Building, University of Oxford, Oxford, OX3 7FZ, UK.; The Francis Crick Institute, London, NW1 1AT, UK., Schofield CJ; Department of Chemistry, University of Oxford Chemistry Research Laboratory, 12 Mansfield Road, Oxford, OX1 3TA, UK.
Jazyk:	angličtina
Zdroj:	ChemMedChem [ChemMedChem] 2020 Feb 05; Vol. 15 (3), pp. 270-273. Date of Electronic Publication: 2019 Dec 03.
DOI:	10.1002/cmdc.201900557
Abstrakt:	The 2-oxoglutarate-dependent hypoxia inducible factor prolyl hydroxylases (PHDs) are targets for treatment of a variety of diseases including anaemia. One PHD inhibitor is approved for use for the treatment of renal anaemia and others are in late stage clinical trials. The number of reported templates for PHD inhibition is limited. We report structure-activity relationship and crystallographic studies on a promising class of 4-hydroxypyrimidine-containing PHD inhibitors. (© 2019 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.)
Databáze:	MEDLINE
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