Discovery of a novel indole series of EP1 receptor antagonists by scaffold hopping

We describe the medicinal chemistry approach that generated a novel indole series of EP(1) receptor antagonists. The SAR of this new template was evaluated and culminated in the identification of compound 12g which demonstrated in vivo efficacy in a preclinical model of inflammatory pain.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2008-04, Vol.18 (8), p.2684-2690
Hauptverfasser:	HALL, Adrian, BILLINTON, Andy, THEOBALD, Pamela J, BROWN, Susan H, CHOWDHURY, Anita, GIBLIN, Gerard M. P, GOLDSMITH, Paul, HURST, David N, NAYLOR, Alan, PATEL, Sadhana, SCOCCITTI, Tiziana
Format:	Artikel
Sprache:	eng
Schlagworte:	Analgesics Animals Biological and medical sciences Humans Hydrogen Bonding Indoles - chemical synthesis Indoles - chemistry Indoles - pharmacology Medical sciences Microsomes, Liver - drug effects Microsomes, Liver - metabolism Models, Molecular Molecular Structure Neuropharmacology Pharmacology. Drug treatments Rats Receptors, Prostaglandin E - antagonists & inhibitors Receptors, Prostaglandin E - metabolism Receptors, Prostaglandin E, EP1 Subtype Structure-Activity Relationship Thiazoles - chemistry
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Beschreibung
Zusammenfassung:	We describe the medicinal chemistry approach that generated a novel indole series of EP(1) receptor antagonists. The SAR of this new template was evaluated and culminated in the identification of compound 12g which demonstrated in vivo efficacy in a preclinical model of inflammatory pain.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2008.03.018