Synthesis and biological evaluation of 3-[4-(amino/methylsulfonyl)phenyl]methylene-indolin-2-one derivatives as novel COX-1/2 and 5-LOX inhibitors.
Bioorg Med Chem Lett
; 20(24): 7349-53, 2010 Dec 15.
Article
en En
| MEDLINE
| ID: mdl-21055929
ABSTRACT
Fourteen new 3-[4-(amino/methylsulfonyl)phenyl]methylene-indolin-2-one derivatives were synthesized. Six compounds displayed potent inhibitory activities against COX-1/2 and 5-LOX with IC(50) in the range of 0.10-9.87 µM. Particularly, 10f exhibited well balanced inhibitory action on these enzymes (IC(50)=0.10-0.56 µM). More importantly, 10f and several other compounds had comparable or stronger anti-inflammatory and analgesic activities, but better gastric tolerability in vivo, as compared with darbufelone mesilate and tenidap sodium. Therefore, our findings may aid in the design of new and safe anti-inflammatory reagents for the intervention of painful inflammatory diseases, such as rheumatoid arthritis at clinic.
Texto completo:
1
Bases de datos:
MEDLINE
Asunto principal:
Compuestos de Bencilideno
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Araquidonato 5-Lipooxigenasa
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Inhibidores de la Lipooxigenasa
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Inhibidores de la Ciclooxigenasa
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Ciclooxigenasa 1
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Ciclooxigenasa 2
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Inhibidores de la Ciclooxigenasa 2
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Indoles
Límite:
Animals
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2010
Tipo del documento:
Article