Bioorganic & Medicinal Chemistry Letters 2006-11-01

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

Namal C Warshakoon, Shengde Wu, Angelique Boyer, Richard Kawamoto, Justin Sheville, Sean Renock, Kevin Xu, Matthew Pokross, Artem G Evdokimov, Richard Walter, Marlene Mekel

Index: Bioorg. Med. Chem. Lett. 16(21) , 5598-601, (2006)

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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.