SAR-study on a new class of imidazo[1,2-a]pyridine-based inhibitors of 5-lipoxygenase.
Bioorg Med Chem Lett
; 22(5): 1969-75, 2012 Mar 01.
Article
em En
| MEDLINE
| ID: mdl-22326163
ABSTRACT
A novel class of 5-lipoxygenase (5-LO) inhibitors characterized by a central imidazo[1,2-a]pyridine scaffold, a cyclohexyl moiety and an aromatic system, is presented. This scaffold was identified in a virtual screening study and exhibits promising inhibitory potential on the 5-LO. Here, we investigate the structure-activity relationships of this compound class. With N-cyclohexyl-6-methyl-2-(4-morpholinophenyl)imidazo[1,2-a]pyridine-3-amine (14), we identified a potent 5-LO inhibitor (IC(50)=0.16µM (intact cells) and 0.1µM (cell-free)), which may possess potential as an effective lead compound intervening with inflammatory diseases and certain types of cancer.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Piridinas
/
Araquidonato 5-Lipoxigenase
/
Inibidores de Lipoxigenase
Limite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2012
Tipo de documento:
Article
País de afiliação:
Alemanha