title: A novel series of imidazo[1,2-a]pyridine derivatives as HIF-1alpha prolyl hydroxylase inhibitors.
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.
authors.affiliation: Procter and Gamble Pharmaceuticals, Inc., 8700 Mason-Montgomery Road, Mason, OH 45040, USA. Warshakoon.nc@pg.com
authors.forename: Namal C
authors.initials: NC
authors.lastname: Warshakoon
authors.forename: Shengde
authors.initials: S
authors.lastname: Wu
authors.forename: Angelique
authors.initials: A
authors.lastname: Boyer
authors.forename: Richard
authors.initials: R
authors.lastname: Kawamoto
authors.forename: Justin
authors.initials: J
authors.lastname: Sheville
authors.forename: Sean
authors.initials: S
authors.lastname: Renock
authors.forename: Kevin
authors.initials: K
authors.lastname: Xu
authors.forename: Matthew
authors.initials: M
authors.lastname: Pokross
authors.forename: Artem G
authors.initials: AG
authors.lastname: Evdokimov
authors.forename: Richard
authors.initials: R
authors.lastname: Walter
authors.forename: Marlene
authors.initials: M
authors.lastname: Mekel
mesh_terms: D006801:Humans; D064799:Hypoxia-Inducible Factor-Proline Dioxygenases; D011393:Procollagen-Proline Dioxygenase / Q000037:antagonists & inhibitors*; D011725:Pyridines / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D011725:Pyridines; C490190:EGLN1 protein, human; D011393:Procollagen-Proline Dioxygenase; D064799:Hypoxia-Inducible Factor-Proline Dioxygenases; C001439:imidazo(1,2-a)pyridine