Studies on spiro[4.5]decanone prolyl hydroxylase domain inhibitors

Autor:	Holt-Martyn, J, Tumber, A, Rahman, M, Lippl, K, Figg, W, McDonough, M, Chowdhury, R, Schofield, C
Rok vydání:	2019
Předmět:	hemic and lymphatic diseases education
Zdroj:	MedChemComm. 2019(4)
ISSN:	2040-2511 2040-2503
Popis:	The 2-oxoglutarate (2OG) dependent hypoxia inducible factor (HIF) prolyl hydroxylases (PHDs) are targets for treatment of anaemia and other ischaemia related diseases. PHD inhibitors are in clinical trials; however, the number of reported templates for PHD inhibition is limited. We report structure–activity relationship and crystallographic studies on spiro[4.5]decanone containing PHD inhibitors. Together with other studies, our results reveal spiro[4.5]decanones as useful templates for generation of potent and selective 2OG oxygenase inhibitors.
Databáze:	OpenAIRE
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