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Naphthalene/quinoline amides and sulfonylureas as potent and selective antagonists of the EP4 receptor

✍ Scribed by Jason D. Burch; Julie Farand; John Colucci; Claudio Sturino; Yves Ducharme; Richard W. Friesen; Jean-François Lévesque; Sébastien Gagné; Mark Wrona; Alex G. Therien; Marie-Claude Mathieu; Danielle Denis; Erika Vigneault; Daigen Xu; Patsy Clark; Steve Rowland; Yongxin Han

Publisher
Elsevier Science
Year
2011
Tongue
English
Weight
755 KB
Volume
21
Category
Article
ISSN
0960-894X

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✦ Synopsis

Two new series of EP(4) antagonists based on naphthalene/quinoline scaffolds have been identified as part of our on-going efforts to develop treatments for inflammatory pain. One series contains an acidic sulfonylurea pharmacophore, whereas the other is a neutral amide. Both series show subnanomolar intrinsic binding potency towards the EP(4) receptor, and excellent selectivity towards other prostanoid receptors. While the amide series generally displays poor pharmacokinetic parameters, the sulfonylureas exhibit greatly improved profile. MF-592, the optimal compound from the sulfonylurea series, has a desirable overall preclinical profile that suggests it is suitable for further development.

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