Discovery of highly selective EP4 receptor agonists that stimulate new bone formation and restore bone mass in ovariectomized rats.
Bioorg Med Chem Lett
; 16(7): 1799-802, 2006 Apr 01.
Article
en En
| MEDLINE
| ID: mdl-16442794
ABSTRACT
Heptanoic acid lactams, exemplified by 2, were identified as highly selective EP4 agonists via high throughput screening. Lead optimization led to the identification of lactams with a 30-fold increase in EP4 potency in vitro. Compounds demonstrated robust bone anabolic effects when administered in vivo in rat models of osteoporosis.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Tamaño de los Órganos
/
Huesos
/
Desarrollo Óseo
/
Ovariectomía
/
Densidad Ósea
/
Receptores de Prostaglandina E
Límite:
Animals
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2006
Tipo del documento:
Article
País de afiliación:
Estados Unidos