Ribeiro Nigel, Tabaka Helena, Peluso Jean, Fetzer Ludivine, Nebigil Can, Dumont Serge, Muller Christian D, Désaubry Laurent
UMR 7175 LC1, ULP-CNRS, Faculté de Pharmacie, 67401 Illkirch, France.
Bioorg Med Chem Lett. 2007 Oct 15;17(20):5523-4. doi: 10.1016/j.bmcl.2007.08.036. Epub 2007 Aug 21.
We synthesized 3-O-methylviridicatin and several analogues of this fungal metabolite. We showed that replacement of the methoxy moiety by a thiomethyl enhanced dramatically its ability to inhibit TNF-alpha secretion. These results strongly suggest that 4-phenyl-3-methylthioquinolinone may provide the basis for the development of new anti-inflammatory agents.
我们合成了3 - O - 甲基绿胶霉素及其几种这种真菌代谢产物的类似物。我们发现，用硫甲基取代甲氧基部分可显著增强其抑制肿瘤坏死因子 - α分泌的能力。这些结果有力地表明，4 - 苯基 - 3 - 甲硫基喹啉酮可能为开发新型抗炎药物提供基础。
