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ID: ALA1138875

Journal: Bioorg Med Chem Lett

Title: Design and synthesis of substituted pyridine derivatives as HIF-1alpha prolyl hydroxylase inhibitors.

Authors: Warshakoon NC, Wu S, Boyer A, Kawamoto R, Sheville J, Bhatt RT, Renock S, Xu K, Pokross M, Zhou S, Walter R, Mekel M, Evdokimov AG, East S.

Abstract: Structure-guided de novo drug design led to the identification of a novel series of substituted pyridine derivatives as HIF-1alpha 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.

CiteXplore: 16908149

DOI: 10.1016/j.bmcl.2006.08.026