1 Ocak 2020 Dergi makalesi Açık Erişim

Celik, Ismail; Erol, Meryem; Puskullu, Mustafa Orhan; Uzunhisarcikli, Ebru; Ince, Ufuk; Kuyucuklu, Gulcan; Suzen, Sibel

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{
  "@context": "https://schema.org/", 
  "@id": 3889, 
  "@type": "ScholarlyArticle", 
  "creator": [
    {
      "@type": "Person", 
      "name": "Celik, Ismail"
    }, 
    {
      "@type": "Person", 
      "affiliation": "Erciyes Univ, Fac Pharm, Dept Pharmaceut Chem, TR-38039 Kayseri, Turkey", 
      "name": "Erol, Meryem"
    }, 
    {
      "@type": "Person", 
      "affiliation": "Erciyes Univ, Fac Pharm, Dept Pharmaceut Chem, TR-38039 Kayseri, Turkey", 
      "name": "Puskullu, Mustafa Orhan"
    }, 
    {
      "@type": "Person", 
      "affiliation": "Erciyes Univ, Fac Pharm, Dept Pharmacol, Kayseri, Turkey", 
      "name": "Uzunhisarcikli, Ebru"
    }, 
    {
      "@type": "Person", 
      "affiliation": "Erciyes Univ, Fac Pharm, Dept Pharmaceut Microbiol, Kayseri, Turkey", 
      "name": "Ince, Ufuk"
    }, 
    {
      "@type": "Person", 
      "affiliation": "Trakya Univ, Fac Med, Dept Med Microbiol, Edirne, Turkey", 
      "name": "Kuyucuklu, Gulcan"
    }, 
    {
      "@type": "Person", 
      "affiliation": "Ankara Univ, Fac Pharm, Dept Pharmaceut Chem, Ankara, Turkey", 
      "name": "Suzen, Sibel"
    }
  ], 
  "datePublished": "2020-01-01", 
  "description": "We previously synthesized a series of quinoline-2-carbaldehyde hydrazone derivatives and evaluated their antioxidant activities. In this study, the antimicrobial activities of these quinoline-2-carbaldehyde hydrazone derivatives were evaluated antimicrobial activity by the microdilution method, and there cytotoxic effect was investigated in MCF-7 and A549 cells by MTT assay. When the activity results were examined, although the antimicrobial activity of quinoline derivatives were equal or better than standard drugs in general, compound4(2 mu g/mL) and8(1 mu g/mL) againstE. faecalisand5(8 mu g/mL) againstP. aeruginosaare the most effective derivatives of the series. Besides, disk diffusion test was applied to these three compounds, and significant zone formation was observed at8(7 mm) compared to vancomycin (9 mm). Compounds showed no antiproliferative in A549 and MCF-7 cell lines, and compound4, 5,and8, which showed the most effective antimicrobial activity, were examined in healthy cells (Beas-2b) and no effect on cell viability was found. To understand the mechanism of this action of these compounds againstE. faecalis, molecular docking studies were performed on 15 different proteins, and it was concluded that the compounds interacted with FabH and not enough with other protein structures. The theoretical ADME profiles of compounds comply with Lipinski and other limiting rules. Also, some theoretical quantum parameters (HOMO-LUMO) of compounds, and both MEP analysis and geometric optimization analysis of8were calculated with 6-311 G (d,p) base set and DFT/B3LYP theory, and the results were shown.", 
  "headline": "In VitroandIn SilicoStudies of Quinoline-2-Carbaldehyde Hydrazone Derivatives as Potent Antimicrobial Agents", 
  "identifier": 3889, 
  "image": "https://aperta.ulakbim.gov.tr/static/img/logo/aperta_logo_with_icon.svg", 
  "license": "http://www.opendefinition.org/licenses/cc-by", 
  "name": "In VitroandIn SilicoStudies of Quinoline-2-Carbaldehyde Hydrazone Derivatives as Potent Antimicrobial Agents", 
  "url": "https://aperta.ulakbim.gov.tr/record/3889"
}