CCR2 receptor antagonists: optimization of biaryl sulfonamides to increase activity in whole blood.
Bioorg Med Chem Lett
; 21(24): 7291-4, 2011 Dec 15.
Article
em En
| MEDLINE
| ID: mdl-22047688
ABSTRACT
A series of biarylsulfonamides was identified as hCCR2 receptor antagonist but suffered from high plasma protein binding resulting in a >100 fold shift in activity in a functional GTPγS assay run in tandem in the presence and absence of human serum albumin. Introduction of an aryl amide with ethylenediamine linker led to compounds with reduced shifts and improved activity in whole blood.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Sulfonamidas
/
Receptores CCR2
Limite:
Animals
/
Humans
Idioma:
En
Ano de publicação:
2011
Tipo de documento:
Article