Discovery of 4-[1-[([1-[4-(trifluoromethyl)benzyl]-1H-indol-7-yl]carbonyl)amino]cyclopropyl]benzoic acid (MF-766), a highly potent and selective EP4 antagonist for treating inflammatory pain

The discovery of a highly potent and selective EP(4) antagonist MF-766 is discussed. This N-benzyl indole derivative exhibits good pharmacokinetic profile and unprecedented in vivo potency in the rat AIA model.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2010-06, Vol.20 (12), p.3760-3763
Hauptverfasser:	Colucci, John, Boyd, Michael, Berthelette, Carl, Chiasson, Jean-Francois, Wang, Zhaoyin, Ducharme, Yves, Friesen, Rick, Wrona, Mark, Levesque, Jean-Francois, Denis, Danielle, Mathieu, Marie-Claude, Stocco, Rino, Therien, Alex G, Clarke, Patsy, Rowland, Steve, Xu, Daigen, Han, Yongxin
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Arthritis - drug therapy Benzoates - chemistry Benzoates - pharmacology Benzoates - therapeutic use Cells, Cultured Dogs Drug Discovery Drug Stability Hepatocytes Humans Indoles - chemistry Indoles - pharmacology Indoles - therapeutic use Inflammation - drug therapy Pain - drug therapy Pharmacokinetics Rats Receptors, Prostaglandin E - antagonists & inhibitors Receptors, Prostaglandin E, EP4 Subtype Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	The discovery of a highly potent and selective EP(4) antagonist MF-766 is discussed. This N-benzyl indole derivative exhibits good pharmacokinetic profile and unprecedented in vivo potency in the rat AIA model.
ISSN:	1464-3405
DOI:	10.1016/j.bmcl.2010.04.065