Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ankara University, 06100 Tandogan, Ankara, Turkey.
Eur J Med Chem. 2011 Feb;46(2):468-79. doi: 10.1016/j.ejmech.2010.11.021. Epub 2010 Nov 26.
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.
在这项研究中,合成了新型 N-(3,5,5,8,8-五甲基-5,6,7,8-四氢萘-2-基)-羧酰胺(6-15)和 5,5,8,8-四甲基-5,6,7,8-四氢萘-2-甲酰胺(16-32)衍生物,并测定了它们在 5μM 和 50μM 浓度下对脂多糖(LPS)激活的 RAW 264.7 巨噬细胞增殖和一氧化氮(NO*)产生的体外影响。发现化合物 12、17、24 和 26 以剂量依赖的方式降低 LPS 激活细胞中的亚硝酸盐水平。在测试的浓度下,这些化合物没有表现出细胞毒性作用。有趣的是,含有氮氧自由基的化合物 27 是该系列中最活跃的化合物,在 LPS 激活的巨噬细胞中表现出 59.2%的亚硝酸盐抑制作用。