Novel methylene-linked heterocyclic EP1 receptor antagonists

We describe the SAR, in terms of heterocyclic replacements, for a series of pyrazole EP(1) receptor antagonists. This study led to the identification of several aromatic heterocyclic replacements for the pyrazole in the original compound. Investigation of replacements for the methylene linker uncove...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2008-03, Vol.18 (5), p.1592-1597
Hauptverfasser:	HALL, Adrian, BIT, Rino A, BROWN, Susan H, CHOWDHURY, Anita, GIBLIN, Gerard M. P, HURST, David N, KILFORD, Ian R, LEWELL, Xiao, NAYLOR, Alan, SCOCCITTI, Tiziana
Format:	Artikel
Sprache:	eng
Schlagworte:	Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Heterocyclic Compounds - chemistry Heterocyclic Compounds - pharmacology Medical sciences Models, Molecular Molecular Structure Pharmacology. Drug treatments Protein Binding Receptors, Prostaglandin E - antagonists & inhibitors Receptors, Prostaglandin E, EP1 Subtype Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	We describe the SAR, in terms of heterocyclic replacements, for a series of pyrazole EP(1) receptor antagonists. This study led to the identification of several aromatic heterocyclic replacements for the pyrazole in the original compound. Investigation of replacements for the methylene linker uncovered disparate SAR in the thiazole and pyridine series.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2008.01.071