1 Ocak 2021 Dergi makalesi Açık Erişim

Dincel, Efe Dogukan; Hasbal-Celikok, Gozde; Yilmaz-Ozden, Tugba; Ulusoy-Guzeldemirci, Nuray

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  "@context": "https://schema.org/", 
  "@id": 239134, 
  "@type": "ScholarlyArticle", 
  "creator": [
    {
      "@type": "Person", 
      "name": "Dincel, Efe Dogukan"
    }, 
    {
      "@type": "Person", 
      "affiliation": "Istanbul Univ, Fac Pharm, Dept Biochem, TR-34116 Istanbul, Turkey", 
      "name": "Hasbal-Celikok, Gozde"
    }, 
    {
      "@type": "Person", 
      "affiliation": "Istanbul Univ, Fac Pharm, Dept Biochem, TR-34116 Istanbul, Turkey", 
      "name": "Yilmaz-Ozden, Tugba"
    }, 
    {
      "@type": "Person", 
      "affiliation": "Istanbul Univ, Fac Pharm, Dept Pharmaceut Chem, TR-34116 Istanbul, Turkey", 
      "name": "Ulusoy-Guzeldemirci, Nuray"
    }
  ], 
  "datePublished": "2021-01-01", 
  "description": "Inhibiting the degradation of carbohydrates into glucose is considered to be an effective treatment for type 2 diabetes mellitus. Herein, a series of novel thiosemicarbazide and 1,2,4-triazole-3-thione derivatives of imidazo[2,1-b]thiazole were synthesized and evaluated for their alpha-glucosidase inhibitory activity. Compound 5c (IC50: 4.54 +/- 0.19 mu M) was found approximately 47 times more active than Acarbose (IC50: 214.71 +/- 8.34 mu M). In addition to the in vitro analysis, molecular docking studies were employed to explore the possible binding interactions of the title compounds. Structure-activity relationships, as well as virtual ADME studies, were carried out and a relationship between biological, electronic, and physicochemical qualifications of the target compounds was determined. Consequently, our studies indicated that these imidazo[2,1-b]thiazole derivatives possess the potential of being a novel class of alpha-glucosidase inhibitors. (C) 2021 Elsevier B.V. All rights reserved.", 
  "headline": "Design, biological evaluation, molecular docking study and in silico ADME prediction of novel imidazo[2,1-b]thiazole derivatives as a novel class of alpha-glucosidase inhibitors", 
  "identifier": 239134, 
  "image": "https://aperta.ulakbim.gov.tr/static/img/logo/aperta_logo_with_icon.svg", 
  "license": "http://www.opendefinition.org/licenses/cc-by", 
  "name": "Design, biological evaluation, molecular docking study and in silico ADME prediction of novel imidazo[2,1-b]thiazole derivatives as a novel class of alpha-glucosidase inhibitors", 
  "url": "https://aperta.ulakbim.gov.tr/record/239134"
}