1 Ocak 2019 Dergi makalesi Açık Erişim

Kucukbay, Hasan; Bugday, Nesrin; Kucukbay, F. Zehra; Berrino, Emanuela; Bartolucci, Gianluca; Del Prete, Sonia; Capasso, Clemente; Supuran, Claudiu T.

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  <identifier identifierType="URL">https://aperta.ulakbim.gov.tr/record/71547</identifier>
  <creators>
    <creator>
      <creatorName>Kucukbay, Hasan</creatorName>
      <givenName>Hasan</givenName>
      <familyName>Kucukbay</familyName>
      <affiliation>Inonu Univ, Fac Arts &amp; Sci, Dept Chem, TR-44280 Malatya, Turkey</affiliation>
    </creator>
    <creator>
      <creatorName>Bugday, Nesrin</creatorName>
      <givenName>Nesrin</givenName>
      <familyName>Bugday</familyName>
      <affiliation>Inonu Univ, Fac Arts &amp; Sci, Dept Chem, TR-44280 Malatya, Turkey</affiliation>
    </creator>
    <creator>
      <creatorName>Kucukbay, F. Zehra</creatorName>
      <givenName>F. Zehra</givenName>
      <familyName>Kucukbay</familyName>
      <affiliation>Inonu Univ, Fac Pharm, Dept Basic Pharmaceut Sci, TR-44280 Malatya, Turkey</affiliation>
    </creator>
    <creator>
      <creatorName>Berrino, Emanuela</creatorName>
      <givenName>Emanuela</givenName>
      <familyName>Berrino</familyName>
    </creator>
    <creator>
      <creatorName>Bartolucci, Gianluca</creatorName>
      <givenName>Gianluca</givenName>
      <familyName>Bartolucci</familyName>
    </creator>
    <creator>
      <creatorName>Del Prete, Sonia</creatorName>
      <givenName>Sonia</givenName>
      <familyName>Del Prete</familyName>
      <affiliation>CNR, Ist Biosci &amp; Biorisorse, Via Pietro Castellino 111, Naples, Italy</affiliation>
    </creator>
    <creator>
      <creatorName>Capasso, Clemente</creatorName>
      <givenName>Clemente</givenName>
      <familyName>Capasso</familyName>
      <affiliation>CNR, Ist Biosci &amp; Biorisorse, Via Pietro Castellino 111, Naples, Italy</affiliation>
    </creator>
    <creator>
      <creatorName>Supuran, Claudiu T.</creatorName>
      <givenName>Claudiu T.</givenName>
      <familyName>Supuran</familyName>
    </creator>
  </creators>
  <titles>
    <title>Synthesis And Carbonic Anhydrase Inhibitory Properties Of Novel 4-(2-Aminoethyl)Benzenesulfonamide-Dipeptide Conjugates</title>
  </titles>
  <publisher>Aperta</publisher>
  <publicationYear>2019</publicationYear>
  <dates>
    <date dateType="Issued">2019-01-01</date>
  </dates>
  <resourceType resourceTypeGeneral="Text">Journal article</resourceType>
  <alternateIdentifiers>
    <alternateIdentifier alternateIdentifierType="url">https://aperta.ulakbim.gov.tr/record/71547</alternateIdentifier>
  </alternateIdentifiers>
  <relatedIdentifiers>
    <relatedIdentifier relatedIdentifierType="DOI" relationType="IsIdenticalTo">10.1016/j.bioorg.2018.11.003</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">Thirty novel sulfonamide derivatives incorporating dipeptide were synthesized by facile acylation through benzotriazole mediated reactions and their structures were identified by H-1 NMR, C-13 NMR, MS and FT-IR spectroscopic techniques and elemental analysis. The carbonic anhydrase (CA, EC 4.2.1.1) inhibitory activity of the new compounds was assessed against four human (h) isoforms, hCA I, hCA II, hCA IV and hCA XII. Most of the synthesized compounds showed excellent in vitro carbonic anhydrase inhibitory properties comparable to those of the clinically used drug acetazolamide (AAZ). The new unprotected dipeptide-sulfonamide conjugates showed very effective inhibitory activity, in the low nanomolar range against II and XII, being less effective as hCA I and IV inhibitors. Four of the thirty compounds also showed strong inhibitory activity against hCA XII compared to AAZ.</description>
  </descriptions>
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