Studies on spiro[4.5]decanone prolyl hydroxylase domain inhibitors?
MedChemComm Pub Date: 2019-03-01 DOI: 10.1039/C8MD00548F
Abstract
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.
![Graphical abstract: Studies on spiro[4.5]decanone prolyl hydroxylase domain inhibitors](http://scimg.chem960.com/usr/1/C8MD00548F.jpg)
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Journal Name：MedChemComm
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CAS no.: 89640-58-4
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