Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1397610 | European Journal of Medicinal Chemistry | 2011 | 12 Pages |
In this study, novel N-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalene-2-yl)-carboxamide (6–15) and 5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalene-2-carboxamide (16–32) derivatives were synthesized and their in vitro effects at 5 μM and 50 μM concentrations on proliferation and nitric oxide (NO) production in lipopolysaccharide (LPS) activated RAW 264.7 macrophage cells were determined. Compounds 12, 17, 24 and 26 were found to decrease nitrite levels in a dose-dependent manner in LPS-activated cells. At the tested concentrations, these compounds did not exhibit cytotoxic effects. Interestingly, compound 27 which contains nitroxide free radical was the most active compound in this series showing 59.2% nitrite inhibition in LPS-activated macrophage cells.
Graphical abstractSome novel retinoid derivatives were synthesized and evaluated for their nitric oxide inhibitory activity.Figure optionsDownload full-size imageDownload as PowerPoint slideResearch highlights► Some novel retinoids were synthesized. ► Retinoid analogues have inhibitory effects on iNOS-related NO production. ► Some retinoids did not show cytotoxicity.