1.
Bioorg Med Chem Lett
; 20(16): 4757-61, 2010 Aug 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-20643546
RESUMEN
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.