1.
Bioorg Med Chem Lett
; 17(8): 2376-9, 2007 Apr 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-17337182
RESUMEN
Inhibitors of PDE5 are useful therapeutic agents for treatment of erectile dysfunction. A series of novel xanthine derivatives has been identified as potent inhibitors of PDE5, with good levels of selectivity against other PDE isoforms, including PDE6. Studies in the dog indicate excellent oral bioavailability for compound 21.
Asunto(s)
3',5'-GMP Cíclico Fosfodiesterasas/antagonistas & inhibidores , Xantinas/farmacología , Animales , Disponibilidad Biológica , Bovinos , Fosfodiesterasas de Nucleótidos Cíclicos Tipo 5 , Perros , Inhibidores Enzimáticos/química , Inhibidores Enzimáticos/farmacología , Inhibidores Enzimáticos/uso terapéutico , Disfunción Eréctil/tratamiento farmacológico , Humanos , Concentración 50 Inhibidora , Masculino , Farmacocinética , Isoformas de Proteínas/efectos de los fármacos , Relación Estructura-Actividad , Xantinas/química
2.
Bioorg Med Chem Lett
; 12(18): 2587-90, 2002 Sep 16.
Artículo
en Inglés
| MEDLINE
| ID: mdl-12182866
RESUMEN
In clinical studies, several inhibitors of phosphodiesterase 5 (PDE5) have demonstrated utility in the treatment of erectile dysfunction. We describe herein a series of 8-aryl xanthine derivatives which function as potent PDE5 inhibitors with, in many cases, high levels of selectivity versus other PDE isoforms.