Research Institute for Basic Sciences and Department of Chemistry, College of Sciences, Kyung Hee University, Seoul 130-701, Republic of Korea.
Bioorg Med Chem Lett. 2010 Jan 15;20(2):734-7. doi: 10.1016/j.bmcl.2009.11.067. Epub 2009 Dec 11.
3,4-Diphenyl-substituted 1H-furan-2,5-dione and 1H-pyrrole-2,5-dione derivatives were synthesized and evaluated for the inhibitory activities on LPS-induced PGE(2) production in RAW 264.7 macrophage cells. Both 1H-furan-2,5-dione and 1H-pyrrole-2,5-dione rings as main scaffolds were easily obtained using one of three synthetic methods. Among the compounds investigated, 1H-3-(4-sulfamoylphenyl)-4-phenyl-pyrrole-2,5-dione (6l) showed a strong inhibitory activity (IC(50)=0.61microM) of PGE(2) production.
3,4-二苯基取代的 1H-呋喃-2,5-二酮和 1H-吡咯-2,5-二酮衍生物被合成，并评估了它们对 RAW 264.7 巨噬细胞中 LPS 诱导的 PGE(2)产生的抑制活性。呋喃-2,5-二酮和吡咯-2,5-二酮环作为主要支架，可使用三种合成方法中的一种来轻易获得。在所研究的化合物中，1H-3-(4-磺酰胺基苯基)-4-苯基-吡咯-2,5-二酮（6l）显示出对 PGE(2)产生的强烈抑制活性（IC(50)=0.61μM）。
