Non-acidic pyrazole EP1 receptor antagonists with in vivo analgesic efficacy

Replacement of the carboxylic acid group in a series of previously described methylene-linked pyrazole EP(1) receptor antagonists led to the discovery of amide, reversed amide and carbamate derivatives. Two compounds, 10a and 10b, were identified as brain penetrant compounds and both demonstrated ef...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2008-06, Vol.18 (11), p.3392-3399
Hauptverfasser:	HALL, Adrian, BILLINTON, Andy, NAYLOR, Alan, PASSINGHAM, Barry, WINYARD, Lisa, BROWN, Susan H, CLAYTON, Nicholas M, CHOWDHURY, Anita, GIBLIN, Gerard M. P, GOLDSMITH, Paul, HAYHOW, Thomas G, HURST, David N, KILFORD, Ian R
Format:	Artikel
Sprache:	eng
Schlagworte:	Analgesics Analgesics - chemical synthesis Analgesics - chemistry Analgesics - pharmacology Animals Biological and medical sciences Brain - drug effects Central Nervous System - drug effects Combinatorial Chemistry Techniques Disease Models, Animal Dose-Response Relationship, Drug Medical sciences Molecular Structure Neuropharmacology Pain Measurement Pharmacology. Drug treatments Pyrazoles - chemical synthesis Pyrazoles - chemistry Pyrazoles - pharmacology Rats Receptors, Prostaglandin E - antagonists & inhibitors Receptors, Prostaglandin E, EP1 Subtype Structure-Activity Relationship
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Zusammenfassung:	Replacement of the carboxylic acid group in a series of previously described methylene-linked pyrazole EP(1) receptor antagonists led to the discovery of amide, reversed amide and carbamate derivatives. Two compounds, 10a and 10b, were identified as brain penetrant compounds and both demonstrated efficacy in the CFA model of inflammatory pain.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2008.04.018