Synthesis and carbonic anhydrase inhibitory properties of amino acid - coumarin/quinolinone conjugates incorporating glycine, alanine and phenylalanine moieties

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dc.authoridKUCUKBAY, HASAN/0000-0002-7180-9486
dc.authoridSupuran, Claudiu/0000-0003-4262-0323
dc.authoridKucukbay, Fatumetuzzehra/0000-0001-7784-4138
dc.authorwosidKUCUKBAY, HASAN/A-5050-2019
dc.authorwosidkucukbay, fatumetuzzehra/X-5743-2019
dc.contributor.authorKucukbay, F. Zehra
dc.contributor.authorKucukbay, Hasan
dc.contributor.authorTanc, Muhammet
dc.contributor.authorSupuran, Claudiu T.
dc.date.accessioned2024-08-04T20:42:41Z
dc.date.available2024-08-04T20:42:41Z
dc.date.issued2016
dc.departmentİnönü Üniversitesien_US
dc.description.abstractN-Protected amino acids (Gly, Ala and Phe) were reacted with amino substituted coumarin and quinolinone derivatives, leading to the corresponding N-protected amino acid-coumarin/quinolinone conjugates. The carbonic anhydrase (CA, EC 4.2.1.1) inhibitory activity of the new compounds was assessed against various human (h) isoforms, such as hCA I, hCA II, hCA IV and hCA XII. The quinolinone conjugates were inactive as enzyme inhibitors, whereas the coumarins were ineffective hCA I/II inhibitors (K(I)s>50 mu M) but were submicromolar hCA IV and XII inhibitors, with inhibition constants ranging between 92 nM and 1.19 mu M for hCA IV, and between 0.11 and 0.79 mu M for hCA XII. These coumarin derivatives, as many others reported earlier, thus show an interesting selective inhibitory profile for the membrane-bound over the cytosolic CA isoforms.en_US
dc.description.sponsorshipInonu University, Turkey (BAPB); Universita degli Studi di Firenze, Italyen_US
dc.description.sponsorshipWe thank Inonu University, Turkey (BAPB), and Universita degli Studi di Firenze, Italy, for financial support.en_US
dc.identifier.doi10.3109/14756366.2015.1113173
dc.identifier.endpage1202en_US
dc.identifier.issn1475-6366
dc.identifier.issn1475-6374
dc.identifier.issue6en_US
dc.identifier.pmid26586254en_US
dc.identifier.scopus2-s2.0-84989332094en_US
dc.identifier.scopusqualityQ1en_US
dc.identifier.startpage1198en_US
dc.identifier.urihttps://doi.org/10.3109/14756366.2015.1113173
dc.identifier.urihttps://hdl.handle.net/11616/97518
dc.identifier.volume31en_US
dc.identifier.wosWOS:000385270300042en_US
dc.identifier.wosqualityQ1en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.language.isoenen_US
dc.publisherTaylor & Francis Ltden_US
dc.relation.ispartofJournal of Enzyme Inhibition and Medicinal Chemistryen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/openAccessen_US
dc.subjectCarbonic anhydraseen_US
dc.subjectcoumarinen_US
dc.subjectinhibitoren_US
dc.subjectN-protected amino acid derivativesen_US
dc.titleSynthesis and carbonic anhydrase inhibitory properties of amino acid - coumarin/quinolinone conjugates incorporating glycine, alanine and phenylalanine moietiesen_US
dc.typeArticleen_US

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