Design and synthesis of novel 3-(benzo[d]oxazol-2-yl)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine derivatives as selective G-protein-coupled receptor kinase-2 and -5 inhibitors.
Bioorg Med Chem Lett
; 23(24): 6711-6, 2013 Dec 15.
Article
em En
| MEDLINE
| ID: mdl-24210504
ABSTRACT
G-protein-coupled receptor kinase (GRK)-2 and -5 are emerging therapeutic targets for the treatment of cardiovascular disease. In our efforts to discover novel small molecules to inhibit GRK-2 and -5, a class of compound based on 3-(benzo[d]oxazol-2-yl)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine was identified as a novel hit by high throughput screening campaign. Structural modification of parent benzoxazole scaffolds by introducing substituents on phenyl displayed potent inhibitory activities toward GRK-2 and -5.
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Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Desenho de Fármacos
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Inibidores de Proteínas Quinases
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Quinase 2 de Receptor Acoplado a Proteína G
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Quinase 5 de Receptor Acoplado a Proteína G
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Aminas
Idioma:
En
Ano de publicação:
2013
Tipo de documento:
Article