Synthesis and PGE(2) production inhibition of 1H-furan-2,5-dione and 1H-pyrrole-2,5-dione derivatives

  • Bioorg Med Chem Lett. 2010 Jan 15;20(2):734-7. doi: 10.1016/j.bmcl.2009.11.067.
Jong Taik Moon  1 ,  Ji Young Jeon ,  Hang Ah Park ,  Young-Soo Noh ,  Kyung-Tae Lee ,  Jungahn Kim ,  Dong Joon Choo ,  Jae Yeol Lee
Affiliations
  • 1. Research Institute for Basic Sciences and Department of Chemistry, College of Sciences, Kyung Hee University, Seoul 130-701, Republic of Korea.
PMID: 20004572 DOI: 10.1016/j.bmcl.2009.11.067
Abstract

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.