Synthesis and structure-activity relationships of biarylcarboxamide bis-aminopyrrolidine urea derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1).
Bioorg Med Chem Lett
; 15(14): 3439-45, 2005 Jul 15.
Article
en En
| MEDLINE
| ID: mdl-15950467
ABSTRACT
A novel series of bis-aminopyrrolidine ureas containing either a 4-biphenylcarboxmide or 5-phenyl-2-thiophenecarboxamide group have been identified as potent and functional antagonists of the melanin-concentrating hormone receptor-1. Syntheses and SAR are described, which led to the discovery of compounds with high binding affinity (Ki = 1 nM) for the receptor. Preliminary in vitro metabolic stability data are also reported for key compounds.
Search on Google
Banco de datos:
MEDLINE
Asunto principal:
Pirrolidinas
/
Urea
/
Receptores de Somatostatina
/
Amidas
Límite:
Animals
Idioma:
En
Año:
2005
Tipo del documento:
Article