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

Bioorg Med Chem Lett. 2006 Nov 1;16(21):5598-601. doi: 10.1016/j.bmcl.2006.08.089. Epub 2006 Sep 8.

Abstract

Utilizing modeling information from a recently resolved structure of human HIF-1alpha 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.

MeSH terms

  • Humans
  • Hypoxia-Inducible Factor-Proline Dioxygenases
  • Procollagen-Proline Dioxygenase / antagonists & inhibitors*
  • Pyridines / pharmacology*
  • Structure-Activity Relationship

Substances

  • Pyridines
  • EGLN1 protein, human
  • Procollagen-Proline Dioxygenase
  • Hypoxia-Inducible Factor-Proline Dioxygenases
  • imidazo(1,2-a)pyridine