1 Ocak 2017 Dergi makalesi Açık Erişim

Turner, Tugba B.; Onder, Ferah Comert; Ipek, Hande; Gungor, Tugba; Savranoglu, Seda; Tok, Tugba Taskin; Celik, Ayhan; Ay, Mehmet

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        "affiliation": "Canakkale Onsekiz Mart Univ, Fac Art & Sci, Dept Mol Biol & Genet, TR-17020 Terzioglu, Turkey", 
        "name": "Turner, Tugba B."
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      {
        "affiliation": "Canakkale Onsekiz Mart Univ, Fac Art & Sci, Dept Chem, Nat Prod & Drug Res Lab, TR-17020 Terzioglu, Turkey", 
        "name": "Onder, Ferah Comert"
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        "affiliation": "Canakkale Onsekiz Mart Univ, Fac Art & Sci, Dept Mol Biol & Genet, TR-17020 Terzioglu, Turkey", 
        "name": "Ipek, Hande"
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      {
        "affiliation": "Canakkale Onsekiz Mart Univ, Fac Art & Sci, Dept Chem, Nat Prod & Drug Res Lab, TR-17020 Terzioglu, Turkey", 
        "name": "Gungor, Tugba"
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      {
        "affiliation": "Canakkale Onsekiz Mart Univ, Fac Art & Sci, Dept Mol Biol & Genet, TR-17020 Terzioglu, Turkey", 
        "name": "Savranoglu, Seda"
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      {
        "affiliation": "Gaziantep Univ, Fac Art & Sci, Dept Chem, TR-27310 Sehitkamil, Gaziantep, Turkey", 
        "name": "Tok, Tugba Taskin"
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      {
        "affiliation": "Gebze Tech Univ, Fac Sci, Dept Chem, TR-41400 Gebze, Kocaeli, Turkey", 
        "name": "Celik, Ayhan"
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      {
        "affiliation": "Canakkale Onsekiz Mart Univ, Fac Art & Sci, Dept Chem, Nat Prod & Drug Res Lab, TR-17020 Terzioglu, Turkey", 
        "name": "Ay, Mehmet"
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    "description": "A series of nitro substituted benzamide derivatives were synthesized and evaluated for their potential anti-inflammatory activities in vitro. Firstly, all compounds (1-6) were screened for their inhibitory capacity on LPS induced nitric oxide (NO) production in RAW264.7 macrophages. Compounds 5 and 6 demonstrated significantly high inhibition capacities in a dose-dependent manner with IC50 values of 3.7 and 53 mu M, respectively. These two compounds were also accompanied by no cytotoxicity at the studied concentrations (max 50 mu M) in macrophages. Molecular docking analysis on iNOS revealed that compounds 5 and 6 bind to the enzyme more efficiently compared to other compounds due to having optimum number of nitro groups, orientations and polarizabilities. In addition, 5 and 6 demonstrated distinct regulatory mechanisms for the expression of the iNOS enzyme at the mRNA and protein levels. Specifically, both suppressed expressions of COX-2, IL-1 beta and TNF-alpha significantly, at 10 and 20 mu M. However, only compound 6 significantly and considerably decreased LPS-induced secretion of IL-1 beta and TNF-alpha. These results suggest that compound 6 may be a multi-potent promising lead compound for further optimization in structure and as well as for in vivo validation studies. (C) 2016 Published by Elsevier B.V.", 
    "doi": "10.1016/j.intimp.2016.12.009", 
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    "journal": {
      "pages": "129-139", 
      "title": "INTERNATIONAL IMMUNOPHARMACOLOGY", 
      "volume": "43"
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    "title": "Biological evaluation and molecular docking. studies of nitro benzamide derivatives with respect to in vitro anti-inflammatory activity"
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