1 Ocak 2021 Dergi makalesi Açık Erişim

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

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  <dc:creator>Dincel, Efe Dogukan</dc:creator>
  <dc:creator>Hasbal-Celikok, Gozde</dc:creator>
  <dc:creator>Yilmaz-Ozden, Tugba</dc:creator>
  <dc:creator>Ulusoy-Guzeldemirci, Nuray</dc:creator>
  <dc:date>2021-01-01</dc:date>
  <dc: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.</dc:description>
  <dc:identifier>https://aperta.ulakbim.gov.trrecord/239134</dc:identifier>
  <dc:identifier>oai:aperta.ulakbim.gov.tr:239134</dc:identifier>
  <dc:rights>info:eu-repo/semantics/openAccess</dc:rights>
  <dc:rights>http://www.opendefinition.org/licenses/cc-by</dc:rights>
  <dc:source>JOURNAL OF MOLECULAR STRUCTURE 1245</dc:source>
  <dc: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</dc:title>
  <dc:type>info:eu-repo/semantics/article</dc:type>
  <dc:type>publication-article</dc:type>
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