Discovery of substituted-2,4-dimethyl-(naphthalene-4-carbonyl)amino-benzoic acid as potent and selective EP4 antagonists.

ID: ALA3739413

Journal: Bioorg Med Chem Lett

Title: Discovery of substituted-2,4-dimethyl-(naphthalene-4-carbonyl)amino-benzoic acid as potent and selective EP4 antagonists.

Authors: Blanco MJ, Vetman T, Chandrasekhar S, Fisher MJ, Harvey A, Mudra D, Wang XS, Yu XP, Schiffler MA, Warshawsky AM.

Abstract: A novel series of EP4 antagonists, based on a quinoline scaffold, has been discovered. Medicinal chemistry efforts to optimize the potency of the initial hit are described. A highly potent compound in a clinically relevant human whole blood assay was identified. Selectivity and pharmacokinetic profiles of this compound are discussed.

CiteXplore: 26608552

DOI: 10.1016/j.bmcl.2015.11.023

Patent ID: ┄