Identification of potent, selective, CNS-targeted inverse agonists of the ghrelin receptor.
Bioorg Med Chem Lett
; 23(19): 5410-4, 2013 Oct 01.
Article
en En
| MEDLINE
| ID: mdl-23953189
ABSTRACT
The optimization for selectivity and central receptor occupancy for a series of spirocyclic azetidine-piperidine inverse agonists of the ghrelin receptor is described. Decreased mAChR muscarinic M2 binding was achieved by use of a chiral indane in place of a substituted benzylic group. Compounds with desirable balance of human in vitro clearance and ex vivo central receptor occupancy were discovered by incorporation of heterocycles. Specifically, heteroaryl rings with nitrogen(s) vicinal to the indane linkage provided the most attractive overall properties.
Palabras clave
Texto completo:
1
Base de datos:
MEDLINE
Asunto principal:
Sistema Nervioso Central
/
Receptores de Ghrelina
Tipo de estudio:
Diagnostic_studies
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2013
Tipo del documento:
Article