1,5-Biaryl pyrrole derivatives as EP1 receptor antagonists: Structure-activity relationships of 4- and 5-substituted benzoic acid derivatives.
Bioorg Med Chem Lett
; 17(3): 732-5, 2007 Feb 01.
Article
en En
| MEDLINE
| ID: mdl-17098427
ABSTRACT
This paper details the SAR of 1,5-biaryl pyrrole derivatives with substituents in the 2-, 4-, and 5-positions of the benzoic acid group as EP1 receptor antagonists. Substitution at the 2-position was poorly tolerated, whereas only fluorine was tolerated at the 4-position. In contrast, a range of substituents at the 5-position were discovered which enhanced the in vitro affinity and led to compounds with promising oral exposure. Three derivatives showed efficacy in a preclinical model of inflammatory pain when dosed orally to rats.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Pirroles
/
Benzoatos
/
Receptores de Prostaglandina E
Tipo de estudio:
Etiology_studies
Límite:
Animals
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2007
Tipo del documento:
Article
País de afiliación:
Reino Unido