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
em 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.
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Base de dados:
MEDLINE
Assunto principal:
Pirrolidinas
/
Ureia
/
Receptores de Somatostatina
/
Amidas
Idioma:
En
Ano de publicação:
2005
Tipo de documento:
Article