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

ChemMedChem 2020 Feb 05

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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.

Citation

James P Holt-Martyn, Rasheduzzaman Chowdhury, Anthony Tumber, Tzu-Lan Yeh, Martine I Abboud, Kerstin Lippl, Christopher T Lohans, Gareth W Langley, William Figg, Michael A McDonough, Christopher W Pugh, Peter J Ratcliffe, Christopher J Schofield. Structure-Activity Relationship and Crystallographic Studies on 4-Hydroxypyrimidine HIF Prolyl Hydroxylase Domain Inhibitors. ChemMedChem. 2020 Feb 05;15(3):270-273