Synthesis and in vitro and in vivo anti-inflammatory activity of novel 4-ferrocenylchroman-2-one derivatives.
J Enzyme Inhib Med Chem
; 34(1): 1678-1689, 2019 Dec.
Article
en En
| MEDLINE
| ID: mdl-31530032
ABSTRACT
A series of novel 4-ferrocenylchroman-2-one derivatives were designed and synthesised to discover potent anti-inflammatory agents for treatment of arthritis. All the target compounds had been screened for their anti-inflammatory activity by evaluating the inhibition effect of LPS-induced NO production in RAW 264.7 macrophages. Among them, 4-ferrocenyl-3,4-dihydro-2H-benzo[g]chromen-2-one (3h) was found to be the most potent compound in inhibiting the productions of NO with low toxicity. This compound also exhibited significant inhibition of the productions of IL-6 and TNF-α in RAW 264.7 macrophages. Preliminary mechanism studies indicated that compound 3h could inhibit the activation of LPS-induced NF-κB and MAPKs signalling pathways. The in vivo anti-inflammatory effect of this compound was determined in the rat adjuvant-induced arthritis model.
Palabras clave
Texto completo:
1
Bases de datos:
MEDLINE
Medicinas Complementárias:
Homeopatia
Asunto principal:
Artritis
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Antiinflamatorios no Esteroideos
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FN-kappa B
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Cromonas
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Interleucina-6
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Factor de Necrosis Tumoral alfa
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Proteínas Quinasas Activadas por Mitógenos
Tipo de estudio:
Prognostic_studies
Idioma:
En
Revista:
J Enzyme Inhib Med Chem
Año:
2019
Tipo del documento:
Article