Author/Authors :
Namal C. Warshakoon، نويسنده , , Shengde Wu، نويسنده , , Angelique Boyer، نويسنده , , Richard Kawamoto، نويسنده , , Justin Sheville، نويسنده , , Ritu Tiku Bhatt، نويسنده , , Sean Renock، نويسنده , , Kevin Xu، نويسنده , , Matthew Pokross، نويسنده , , Songtao Zhou، نويسنده , , Richard Walter، نويسنده , , Marlene Mekel، نويسنده , , Artem G. Evdokimov، نويسنده , , Stephen East، نويسنده ,
Abstract :
Structure-guided de novo drug design led to the identification of a novel series of substituted pyridine derivatives as HIF-1α prolyl hydroxylase inhibitors. Pyridine carboxyamide derivatives bearing a substituted aryl group at the 5-position of the pyridine ring show appreciable activity, while constraining the side chain by placing a pyrazole carboxylic acid generated a potent lead series with consistent activity against EGLN-1.
Keywords :
Prolyl hydroxylase inhibitors , HIF-1? , hypoxia , ischemia , Peripheral arterial disease (PAD) , anemia
