Synthesis and potential anti-inflammatory activity of some tetrahydrophthalazinones.
J Enzyme Inhib Med Chem
; 19(6): 475-80, 2004 Dec.
Article
em En
| MEDLINE
| ID: mdl-15662951
ABSTRACT
A solid-phase route for the preparation of 4a,5,8,8a-tetrahydrophthalazinon-1-ones employing the Diels-Alder reaction has been developed. Some of the new compounds have been tested for inhibition of LPS-stimulated TNF-alpha production in human whole blood from patients with chronic obstructive pulmonary disease (COPD). This evaluation revealed two compounds 17 and 18 of interest, incorporating an arylpiperazine moiety, which were found to inhibit LPS-induced TNF-alpha release like the well known anti-inflammatory PDE4 inhibitors, rolipram and roflumilast.
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Base de dados:
MEDLINE
Assunto principal:
Inibidores de Fosfodiesterase
/
Ftalazinas
/
Anti-Inflamatórios não Esteroides
/
Doença Pulmonar Obstrutiva Crônica
Tipo de estudo:
Prognostic_studies
Idioma:
En
Revista:
J Enzyme Inhib Med Chem
Ano de publicação:
2004
Tipo de documento:
Article
País de afiliação:
França