3,4,5-Trisubstituted isoxazoles as novel PPARdelta agonists. Part 2.
Bioorg Med Chem Lett
; 16(21): 5488-92, 2006 Nov 01.
Article
en En
| MEDLINE
| ID: mdl-16931011
ABSTRACT
A series of PPARdelta-selective agonists was investigated and optimized for a favorable in vivo pharmacokinetic profile. Isoxazole LCI765 (17d) was found to be a potent and selective PPARdelta agonist with good in vivo PK properties in mouse (C(max)=5.1 microM, t(1/2)=3.1 h). LCI765 regulated expression of genes involved in energy homeostasis in relevant tissues when dosed orally in C57BL6 mice. A co-crystal structure of compound LCI765 and the LBD of PPARdelta is discussed.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
PPAR delta
/
Isoxazoles
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