Design, synthesis, and PPARalpha/gamma agonistic activity of novel tetrahydroisoquinoline derivatives / 药学学报
Acta Pharmaceutica Sinica
;
(12): 311-316, 2011.
Artículo
en Chino
| WPRIM
| ID: wpr-348959
ABSTRACT
A series of tetrahydroisoquinoline derivatives were prepared and their peroxisome proliferator-activated receptor (PPAR) alpha/gamma agonistic activities were evaluated to obtain more potent PPAR agonist. All of them were new compounds, and their structures were confirmed by 1H NMR and HR-MS. Three compounds exhibited higher agonistic activities of PPARgamma than that of the comparison, six compounds exhibited higher agonistic activities of PPARalpha than that of the comparison, and compound 8a was discovered as a highly potent PPARalpha/gamma agonist that is much more active than that of WY14643 and rosiglitazone. The development of potent PPAR agonists may offer a new choice for the treatment of diabetes.
Texto completo:
Disponible
Índice:
WPRIM (Pacífico Occidental)
Asunto principal:
Farmacología
/
Relación Estructura-Actividad
/
Transfección
/
Diseño de Fármacos
/
Química
/
Tetrahidroisoquinolinas
/
PPAR alfa
/
PPAR gamma
/
Células HEK293
/
Hipoglucemiantes
Límite:
Humanos
Idioma:
Chino
Revista:
Acta Pharmaceutica Sinica
Año:
2011
Tipo del documento:
Artículo
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