1 Ocak 2021 Dergi makalesi Açık Erişim

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

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        "name": "Dincel, Efe Dogukan"
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        "affiliation": "Istanbul Univ, Fac Pharm, Dept Biochem, TR-34116 Istanbul, Turkey", 
        "name": "Hasbal-Celikok, Gozde"
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      {
        "affiliation": "Istanbul Univ, Fac Pharm, Dept Biochem, TR-34116 Istanbul, Turkey", 
        "name": "Yilmaz-Ozden, Tugba"
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        "affiliation": "Istanbul Univ, Fac Pharm, Dept Pharmaceut Chem, TR-34116 Istanbul, Turkey", 
        "name": "Ulusoy-Guzeldemirci, Nuray"
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    "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.", 
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      "title": "JOURNAL OF MOLECULAR STRUCTURE", 
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    "title": "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"
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