Synthesis and cannabinoid-1 receptor binding affinity of conformationally constrained analogs of taranabant.
Bioorg Med Chem Lett
; 20(16): 4757-61, 2010 Aug 15.
Article
en En
| MEDLINE
| ID: mdl-20643546
ABSTRACT
The design, synthesis, and binding activity of ring constrained analogs of the acyclic cannabinoid-1 receptor (CB1R) inverse agonist taranabant 1 are described. The initial inspiration for these taranabant derivatives was its conformation 1a, determined by (1)H NMR, X-ray, and molecular modeling. The constrained analogs were all much less potent than their acyclic parent structure. The results obtained are discussed in the context of a predicted binding of 1 to a homology model of CB1R.
Texto completo:
1
Base de datos:
MEDLINE
Asunto principal:
Piridinas
/
Fármacos Antiobesidad
/
Receptor Cannabinoide CB1
/
Amidas
Tipo de estudio:
Prognostic_studies
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2010
Tipo del documento:
Article