A novel series of imidazo[1,2- a]pyridine derivatives as HIF-1α prolyl hydroxylase inhibitors

Utilizing modeling information from a recently resolved structure of human HIF-1α prolyl hydroxylase (EGLN1) and structure-based design, a novel series of imidazo[1,2- a]pyridine derivatives was prepared. The activity of these compounds was determined in a human EGLN1 assay and a limited SAR was dev...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2006-11, Vol.16 (21), p.5598-5601
Hauptverfasser:	Warshakoon, Namal C., Wu, Shengde, Boyer, Angelique, Kawamoto, Richard, Sheville, Justin, Renock, Sean, Xu, Kevin, Pokross, Matthew, Evdokimov, Artem G., Walter, Richard, Mekel, Marlene
Format:	Artikel
Sprache:	eng
Schlagworte:	Analytical, structural and metabolic biochemistry Biological and medical sciences Enzymes and enzyme inhibitors Fundamental and applied biological sciences. Psychology HIF-1α prolyl hydroxylase inhibitors Imidazo[1,2- a]pyridines Medical sciences Miscellaneous Oxidoreductases Pharmacology. Drug treatments
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Zusammenfassung:	Utilizing modeling information from a recently resolved structure of human HIF-1α prolyl hydroxylase (EGLN1) and structure-based design, a novel series of imidazo[1,2- a]pyridine derivatives was prepared. The activity of these compounds was determined in a human EGLN1 assay and a limited SAR was developed.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2006.08.089