3-Urea-1-(phenylmethyl)-pyridones as novel, potent, and selective EP sub(3) receptor antagonists

A series of 3-urea-1-(phenylmethyl)-pyridones was discovered as novel EP sub(3) antagonists via high-throughput screening and subsequent optimization. The synthesis, structure-activity relationships, and optimization of the initial hit that resulted in potent and selective EP sub(3) receptor antagon...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2010-11, Vol.20 (22), p.6744-6747
Hauptverfasser: Li, Yue H, Tseng, Pei-San, Evans, Karen A, Jaworski, Jon-Paul, Morrow, Dwight M, Fries, Harvey E, Wu, Charlene W, Edwards, Richard M, Jin, Jian
Format: Artikel
Sprache:eng
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Zusammenfassung:A series of 3-urea-1-(phenylmethyl)-pyridones was discovered as novel EP sub(3) antagonists via high-throughput screening and subsequent optimization. The synthesis, structure-activity relationships, and optimization of the initial hit that resulted in potent and selective EP sub(3) receptor antagonists such as 11g are described.
ISSN:0960-894X
DOI:10.1016/j.bmcl.2010.08.137