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