1.
ChemMedChem
; 13(8): 795-802, 2018 04 23.
Artículo
en Inglés
| MEDLINE
| ID: mdl-29451954
RESUMEN
Selective leads: In this study, we generated a new series of serotonin 5-HT7 receptor antagonists. Their synthesis, structure-activity relationships, and selectivity profiles are reported. This series includes 5-HT7 antagonists with unprecedented high selectivity for the 5-HT7 receptor, setting the stage for lead optimization of drugs acting on a range of neurological targets.
Asunto(s)
Receptores de Serotonina/metabolismo , Antagonistas de la Serotonina/química , Antagonistas de la Serotonina/farmacología , Bibliotecas de Moléculas Pequeñas/química , Bibliotecas de Moléculas Pequeñas/farmacología , Células HEK293 , Humanos , Isoquinolinas/química , Isoquinolinas/farmacología , Relación Estructura-Actividad
2.
Bioorg Med Chem Lett
; 19(10): 2780-4, 2009 May 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-19369077
RESUMEN
A series of 4-azaindole inhibitors of c-Met kinase is described. The postulated binding mode was confirmed by an X-ray crystal structure and series optimisation was performed on the basis of this structure. Future directions for series development are discussed.