1.
Bioorg Med Chem Lett
; 20(12): 3742-5, 2010 Jun 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-20471258
RESUMO
A series of biaryl amides containing an azabicyclooctane amine headpiece were synthesized and evaluated as mixed arginine vasopressin (AVP) receptor antagonists. Several analogues, including 8g, 12g, 13d, and 13g, were shown to have excellent V(1a)- and good V(2)-receptor binding affinities. Compound 13d was further profiled for drug-like properties and for an in vitro comparison with conivaptan, the program's mixed V(1a)/V(2)-receptor antagonist standard.