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

[Display omitted] 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 pha...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2016-01, Vol.26 (1), p.105-109
Hauptverfasser:	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.
Format:	Artikel
Sprache:	eng
Schlagworte:	Arthritis pain Benzoates - chemical synthesis Benzoates - chemistry Benzoates - pharmacology Dose-Response Relationship, Drug Drug Discovery EP4 receptor antagonist Human whole blood assay Humans Molecular Structure Naphthalenes - chemical synthesis Naphthalenes - chemistry Naphthalenes - pharmacology Prostaglandin E2 Receptors, Prostaglandin E, EP4 Subtype - antagonists & inhibitors Structure-Activity Relationship
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Zusammenfassung:	[Display omitted] 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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2015.11.023