Discovery of novel biaryl heterocyclic EP1 receptor antagonists

The synthesis and biological activity of a series of novel EP1 receptor antagonists are described. In vitro and in vivo DMPK data are presented for selected compounds. We describe the generation of novel EP1 receptor antagonists by investigation of thiophene isosteres. In addition, we disclose preli...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2006-05, Vol.16 (10), p.2666-2671
Hauptverfasser:	Hall, Adrian, Bit, Rino A., Brown, Susan H., Chaignot, Helene M., Chessell, Iain P., Coleman, Tanya, Giblin, Gerard M.P., Hurst, David N., Kilford, Ian R., Lewell, Xiao Q., Michel, Anton D., Mohamed, Shiyam, Naylor, Alan, Novelli, Riccardo, Skinner, Lee, Spalding, David J., Tang, Sac P., Wilson, Richard J.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological and medical sciences Cyclopentene EP1 antagonist Heterocycles Heterocyclic Compounds - chemistry Heterocyclic Compounds - pharmacology In Vitro Techniques Isostere Medical sciences Miscellaneous Pain Pharmacology. Drug treatments Rats Receptors, Prostaglandin E - antagonists & inhibitors Receptors, Prostaglandin E, EP1 Subtype
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Beschreibung
Zusammenfassung:	The synthesis and biological activity of a series of novel EP1 receptor antagonists are described. In vitro and in vivo DMPK data are presented for selected compounds. We describe the generation of novel EP1 receptor antagonists by investigation of thiophene isosteres. In addition, we disclose preliminary in vitro and in vivo DMPK for selected compounds.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2006.02.014