Phosphodiesterase inhibitors. Part 2: design, synthesis, and structure-activity relationships of dual PDE3/4-inhibitory pyrazolo[1,5-a]pyridines with anti-inflammatory and bronchodilatory activity.
Bioorg Med Chem Lett
; 21(18): 5451-6, 2011 Sep 15.
Article
em En
| MEDLINE
| ID: mdl-21764304
ABSTRACT
A structural survey of pyrazolopyridine-pyridazinone phosphodiesterase (PDE) inhibitors was made with a view to optimization of their dual PDE3/4-inhibitory activity for respiratory disease applications. These studies identified (-)-6-(7-methoxy-2-trifluoromethylpyrazolo[1,5-a]pyridine-4-yl)-5-methyl-4,5-dihydro-3-(2H)-pyridazinone (KCA-1490, compound 2ac) as a compound with potent combined bronchodilatory and anti-inflammatory activity and an improved therapeutic window over roflumilast.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Pirazóis
/
Piridinas
/
Broncodilatadores
/
Desenho de Fármacos
/
Anti-Inflamatórios não Esteroides
/
Inibidores da Fosfodiesterase 3
/
Inibidores da Fosfodiesterase 4
Limite:
Animals
Idioma:
En
Revista:
Bioorg Med Chem Lett
Ano de publicação:
2011
Tipo de documento:
Article