New class of biphenylene dibenzazocinones as potent ligands for the human EP1 prostanoid receptor

A new class of potent and selective ligands for the human EP1 prostanoid receptor is described. SAR studies reported herein allowed the identification of several potent dibenzazocinones bearing an acylsulfonamide side chain. The binding affinity of these compounds on all eight human prostanoid recep...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 1999-09, Vol.9 (18), p.2699-2704
Hauptverfasser:	RUEL, R, LACOMBE, P, LABELLE, M, ABRAMOVITZ, M, GODBOUT, C, LAMONTAGNE, S, ROCHETTE, C, SAWYER, N, STOCCO, R, TREMBLAY, N. M, METTERS, K. M
Format:	Artikel
Sprache:	eng
Schlagworte:	Analgesics Azocines - chemistry Azocines - metabolism Azocines - pharmacology Biological and medical sciences Biphenyl Compounds - chemistry Biphenyl Compounds - metabolism Biphenyl Compounds - pharmacology Humans Ligands Medical sciences Neuropharmacology Pharmacology. Drug treatments Protein Binding Receptors, Prostaglandin E - drug effects Receptors, Prostaglandin E - metabolism Receptors, Prostaglandin E, EP1 Subtype Structure-Activity Relationship
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Zusammenfassung:	A new class of potent and selective ligands for the human EP1 prostanoid receptor is described. SAR studies reported herein allowed the identification of several potent dibenzazocinones bearing an acylsulfonamide side chain. The binding affinity of these compounds on all eight human prostanoid receptors is reported.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/s0960-894x(99)00465-5