Discovery of substituted-2, 4-dimethyl-(naphthalene-4-carbonyl)amino-benzoic acid as potent and selective EP4 antagonists. Issue 1 (1st January 2016)

• Record Type: Journal Article
• Authors: Blanco, Maria-Jesus; Vetman, Tatiana; Chandrasekhar, Srinivasan; Fisher, Matthew J.; Harvey, Anita; Mudra, Daniel; Wang, Xu-Shan; Yu, Xiao-Peng; Schiffler, Matthew A.; Warshawsky, Alan M.
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 1(2016)
• Page Start: 105
• Page End: 109
• Publication Date: 2016-01-01
• Subjects: Arthritis pain -- EP4 receptor antagonist -- Prostaglandin E2 -- Human whole blood assay; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2015.11.023
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: 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.