1 Ocak 2021 Dergi makalesi Açık Erişim

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

DataCite XML

<?xml version='1.0' encoding='utf-8'?>
<resource xmlns:xsi="http://www.w3.org/2001/XMLSchema-instance" xmlns="http://datacite.org/schema/kernel-4" xsi:schemaLocation="http://datacite.org/schema/kernel-4 http://schema.datacite.org/meta/kernel-4.1/metadata.xsd">
  <identifier identifierType="URL">https://aperta.ulakbim.gov.tr/record/239134</identifier>
  <creators>
    <creator>
      <creatorName>Dincel, Efe Dogukan</creatorName>
      <givenName>Efe Dogukan</givenName>
      <familyName>Dincel</familyName>
    </creator>
    <creator>
      <creatorName>Hasbal-Celikok, Gozde</creatorName>
      <givenName>Gozde</givenName>
      <familyName>Hasbal-Celikok</familyName>
      <affiliation>Istanbul Univ, Fac Pharm, Dept Biochem, TR-34116 Istanbul, Turkey</affiliation>
    </creator>
    <creator>
      <creatorName>Yilmaz-Ozden, Tugba</creatorName>
      <givenName>Tugba</givenName>
      <familyName>Yilmaz-Ozden</familyName>
      <affiliation>Istanbul Univ, Fac Pharm, Dept Biochem, TR-34116 Istanbul, Turkey</affiliation>
    </creator>
    <creator>
      <creatorName>Ulusoy-Guzeldemirci, Nuray</creatorName>
      <givenName>Nuray</givenName>
      <familyName>Ulusoy-Guzeldemirci</familyName>
      <affiliation>Istanbul Univ, Fac Pharm, Dept Pharmaceut Chem, TR-34116 Istanbul, Turkey</affiliation>
    </creator>
  </creators>
  <titles>
    <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</title>
  </titles>
  <publisher>Aperta</publisher>
  <publicationYear>2021</publicationYear>
  <dates>
    <date dateType="Issued">2021-01-01</date>
  </dates>
  <resourceType resourceTypeGeneral="Text">Journal article</resourceType>
  <alternateIdentifiers>
    <alternateIdentifier alternateIdentifierType="url">https://aperta.ulakbim.gov.tr/record/239134</alternateIdentifier>
  </alternateIdentifiers>
  <relatedIdentifiers>
    <relatedIdentifier relatedIdentifierType="DOI" relationType="IsIdenticalTo">10.1016/j.molstruc.2021.131260</relatedIdentifier>
  </relatedIdentifiers>
  <rightsList>
    <rights rightsURI="http://www.opendefinition.org/licenses/cc-by">Creative Commons Attribution</rights>
    <rights rightsURI="info:eu-repo/semantics/openAccess">Open Access</rights>
  </rightsList>
  <descriptions>
    <description descriptionType="Abstract">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.</description>
  </descriptions>
</resource>