Studies on spiro[4.5]decanone prolyl hydroxylase domain inhibitors.
Medchemcomm
; 10(4): 500-504, 2019 Apr 01.
Article
em En
| MEDLINE
| ID: mdl-31057728
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.
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1
Coleções:
01-internacional
Base de dados:
MEDLINE
Idioma:
En
Revista:
Medchemcomm
Ano de publicação:
2019
Tipo de documento:
Article