TNF-α and IL-6 inhibitors: Conjugates of N-substituted indole and aminophenylmorpholin-3-one as anti-inflammatory agents.
Eur J Med Chem
; 140: 92-103, 2017 Nov 10.
Article
em En
| MEDLINE
| ID: mdl-28923390
ABSTRACT
The conjugates obtained by the combination of indole and aminophenyl morpholinone were screened for TNF-α and IL-6 inhibition in microglial cells. Compound 4 was found to be the most potent anti-inflammatory agent as it reduced LPS induced level of inflammatory cytokines TNF-α and IL-6 by 71% and 53%, respectively. A significant decrease in NO and MMPs release from BV2 cells in culture pretreated with this compound as well as inhibition of nuclear translocation of NF-κB and AP-1 was observed. 75% inhibition of acetic acid induced algesia in swiss albino mice was noticed in the presence of compound 4. Experimental data and molecular docking studies indicate that the compounds are targeting TNF-α, iNOS and IL-6.
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Base de dados:
MEDLINE
Assunto principal:
Anti-Inflamatórios não Esteroides
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Morfolinas
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Interleucina-6
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Fator de Necrose Tumoral alfa
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Analgésicos
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Indóis
Idioma:
En
Ano de publicação:
2017
Tipo de documento:
Article