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Biological evaluation and molecular docking studies of nitro benzamide derivatives with respect to in vitro anti-inflammatory activity.

Abstract：

:A series of nitro substituted benzamide derivatives were synthesized and evaluated for their potential anti-inflammatory activities in vitro. Firstly, all compounds (1-6) were screened for their inhibitory capacity on LPS induced nitric oxide (NO) production in RAW264.7 macrophages. Compounds 5 and 6 demonstrated significantly high inhibition capacities in a dose-dependent manner with IC50 values of 3.7 and 5.3μM, respectively. These two compounds were also accompanied by no cytotoxicity at the studied concentrations (max 50μM) in macrophages. Molecular docking analysis on iNOS revealed that compounds 5 and 6 bind to the enzyme more efficiently compared to other compounds due to having optimum number of nitro groups, orientations and polarizabilities. In addition, 5 and 6 demonstrated distinct regulatory mechanisms for the expression of the iNOS enzyme at the mRNA and protein levels. Specifically, both suppressed expressions of COX-2, IL-1β and TNF-α significantly, at 10 and 20μM. However, only compound 6 significantly and considerably decreased LPS-induced secretion of IL-1β and TNF-α. These results suggest that compound 6 may be a multi-potent promising lead compound for further optimization in structure and as well as for in vivo validation studies.

journal_name

Int Immunopharmacol

journal_title

International immunopharmacology

authors

Tumer TB,Onder FC,Ipek H,Gungor T,Savranoglu S,Tok TT,Celik A,Ay M

doi

10.1016/j.intimp.2016.12.009

subject

Has Abstract

pub_date

2017-02-01 00:00:00

pages

129-139

eissn

1567-5769

issn

1878-1705

pii

S1567-5769(16)30501-X

journal_volume

43

pub_type

杂志文章

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