Literature DB >> 20004572

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

Jong Taik Moon1, Ji Young Jeon, Hang Ah Park, Young-Soo Noh, Kyung-Tae Lee, Jungahn Kim, Dong Joon Choo, Jae Yeol Lee.   

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. Copyright 2009 Elsevier Ltd. All rights reserved.

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Year:  2009        PMID： 20004572     DOI： 10.1016/j.bmcl.2009.11.067

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  4 in total

1.  Potent anti-inflammatory effect of a novel furan-2,5-dione derivative, BPD, mediated by dual suppression of COX-2 activity and LPS-induced inflammatory gene expression via NF-κB inactivation.

Authors:  Ji-Sun Shin; Seung-Jae Park; Suran Ryu; Han Byul Kang; Tae Woo Kim; Jung-Hye Choi; Jae-Yeol Lee; Young-Wuk Cho; Kyung-Tae Lee
Journal:  Br J Pharmacol       Date:  2012-03       Impact factor: 8.739

2.  Synthesis and biological activity of aminophthalazines and aminopyridazines as novel inhibitors of PGE2 production in cells.

Authors:  Federico Medda; Earlphia Sells; Hui-Hua Chang; Justin Dietrich; Shashi Chappeta; Breland Smith; Vijay Gokhale; Emmanuelle J Meuillet; Christopher Hulme
Journal:  Bioorg Med Chem Lett       Date:  2012-11-21       Impact factor: 2.823

3.  Synthesis and biological activity of 2-aminothiazoles as novel inhibitors of PGE2 production in cells.

Authors:  Breland Smith; Hui-Hua Chang; Federico Medda; Vijay Gokhale; Justin Dietrich; Angela Davis; Emmanuelle J Meuillet; Christopher Hulme
Journal:  Bioorg Med Chem Lett       Date:  2012-03-28       Impact factor: 2.823

4.  Synthesis and Structural Study of Amidrazone Derived Pyrrole-2,5-Dione Derivatives: Potential Anti-Inflammatory Agents.

Authors:  Renata Paprocka; Leszek Pazderski; Liliana Mazur; Małgorzata Wiese-Szadkowska; Jolanta Kutkowska; Michalina Nowak; Anna Helmin-Basa
Journal:  Molecules       Date:  2022-04-30       Impact factor: 4.411
  4 in total

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