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Rosiglitazone has shown promising anti-inflammation effect. To develop preferable anti-inflammatory agents, twenty-two rosiglitazone analogs were synthesized and their anti-inflammatory activity was evaluated. Among these compounds, 6i and 6k displayed excellent inhibitory activities on the production of inflammatory mediators, including nitric oxide (NO), tumor necrosis factor-alpha (TNF-α) and interleukin-6 (IL-6). Furthermore, 6i and 6k showed suppression effects on the nuclear factor-kappa B (NF-κB) and mitogen-activated protein kinase (MAPK) pathways, and this suppression effects could be partially reversed by GW9662, which is a peroxisome proliferator-activated receptor γ (PPARγ) antagonist. Additionally, our docking results exhibited the well combination of 6i and 6k to PPARγ. So the anti-inflammation activity of 6i and 6k was due at least in part, to their interaction with PPARγ.

Titel:	Design, synthesis and anti-inflammatory evaluation of novel 5-benzylidene-3,4-dihalo-furan-2-one derivatives.
Autor/in / Beteiligte Person:	Wang, F ; Sun, JR ; Huang, MY ; Wang, HY ; Sun, PH ; Lin, J ; Chen, WM
Link:	Zum Volltext
Zeitschrift:	European journal of medicinal chemistry, Jg. 72 (2014-01-24), S. 35
Veröffentlichung:	Paris : Editions Scientifiques Elsevier ; <i>Original Publication</i>: Paris, S.E.C.T. [etc.], 2014
Medientyp:	academicJournal
ISSN:	1768-3254 (electronic)
DOI:	10.1016/j.ejmech.2013.10.074
Schlagwort:	Anilides pharmacology Animals Anti-Inflammatory Agents, Non-Steroidal chemical synthesis Anti-Inflammatory Agents, Non-Steroidal chemistry Benzylidene Compounds chemical synthesis Benzylidene Compounds chemistry Cell Line Cell Survival Furans chemical synthesis Furans chemistry Interleukin-6 biosynthesis Mice Mitogen-Activated Protein Kinases metabolism Models, Molecular Molecular Structure NF-kappa B metabolism Nitric Oxide biosynthesis Structure-Activity Relationship Tumor Necrosis Factor-alpha biosynthesis Anti-Inflammatory Agents, Non-Steroidal pharmacology Benzylidene Compounds pharmacology Drug Design Furans pharmacology Interleukin-6 antagonists & inhibitors Mitogen-Activated Protein Kinases antagonists & inhibitors NF-kappa B antagonists & inhibitors Nitric Oxide antagonists & inhibitors Tumor Necrosis Factor-alpha antagonists & inhibitors
Sonstiges:	Nachgewiesen in: MEDLINE Sprachen: English Publication Type: Journal Article; Research Support, Non-U.S. Gov't Language: English [Eur J Med Chem] 2014 Jan 24; Vol. 72, pp. 35-45. <i>Date of Electronic Publication: </i>2013 Nov 20. MeSH Terms: Drug Design* ; Anti-Inflammatory Agents, Non-Steroidal / pharmacology ; Benzylidene Compounds / pharmacology ; Furans / pharmacology ; Interleukin-6 / antagonists & inhibitors ; Mitogen-Activated Protein Kinases / antagonists & inhibitors ; NF-kappa B / antagonists & inhibitors ; Nitric Oxide / antagonists & inhibitors ; Tumor Necrosis Factor-alpha / antagonists & inhibitors ; Anilides / pharmacology ; Animals ; Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis ; Anti-Inflammatory Agents, Non-Steroidal / chemistry ; Benzylidene Compounds / chemical synthesis ; Benzylidene Compounds / chemistry ; Cell Line ; Cell Survival ; Furans / chemical synthesis ; Furans / chemistry ; Interleukin-6 / biosynthesis ; Mice ; Mitogen-Activated Protein Kinases / metabolism ; Models, Molecular ; Molecular Structure ; NF-kappa B / metabolism ; Nitric Oxide / biosynthesis ; Structure-Activity Relationship ; Tumor Necrosis Factor-alpha / biosynthesis Contributed Indexing: Keywords: 3,4-Dihalo-furan-2-one; ABANBEMMKJDTOF-PTNGSMBKSA-N; AMJIFQUYNVDTFW-IUXPMGMMSA-N; Action mechanism; Anti-inflammation; CHJVOYRHJNNIMW-YBEGLDIGSA-N; CIOUHMMWGSCAGE-BOPFTXTBSA-N; CXIOINFZWKMBRE-PXNMLYILSA-N; FHKOJWSHWJJAGD-YBEGLDIGSA-N; FKOSYLLHVHNTSB-WQRHYEAKSA-N; IVHUDKIIJMQQPF-PXNMLYILSA-N; JNMWXEAYOCCTNX-ZROIWOOFSA-N; JTLWBBCUDCJUMW-IUXPMGMMSA-N; KAFDGUUQEAQRRD-WJDWOHSUSA-N; LGZKLGBJPAHGJM-NVMNQCDNSA-N; LZGWJKGHJBSCEQ-UNOMPAQXSA-N; MHQROZUURSCCLO-ATVHPVEESA-N; NXVJMBQJUQBQJO-ATVHPVEESA-N; PPARγ; QRNWQFRSONLXNU-ZROIWOOFSA-N; QWIPTCMHCFLGIV-WJDWOHSUSA-N; RWIGBEAPQKJRPF-BOPFTXTBSA-N; Synthesis; TVOYMUJQDNCTLS-DHDCSXOGSA-N; WSYCMIWDSXXXAD-DHDCSXOGSA-N; YJWGLMMFJLJYGT-PXNMLYILSA-N; YJYLUYMSVPTCOU-PTNGSMBKSA-N Substance Nomenclature: 0 (2-chloro-5-nitrobenzanilide) ; 0 (Anilides) ; 0 (Anti-Inflammatory Agents, Non-Steroidal) ; 0 (Benzylidene Compounds) ; 0 (Furans) ; 0 (Interleukin-6) ; 0 (NF-kappa B) ; 0 (Tumor Necrosis Factor-alpha) ; 31C4KY9ESH (Nitric Oxide) ; EC 2.7.11.24 (Mitogen-Activated Protein Kinases) Entry Date(s): Date Created: 20131217 Date Completed: 20141125 Latest Revision: 20140203 Update Code: 20240513

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Design, synthesis and anti-inflammatory evaluation of novel 5-benzylidene-3,4-dihalo-furan-2-one derivatives.