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TNF-α and IL-6 inhibitors: Conjugates of N-substituted indole and aminophenylmorpholin-3-one as anti-inflammatory agents.

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.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Singh P,Kaur S,Sharma A,Kaur G,Bhatti R

doi

10.1016/j.ejmech.2017.09.003

subject

Has Abstract

pub_date

2017-11-10 00:00:00

pages

92-103

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(17)30685-2

journal_volume

140

pub_type

杂志文章

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