Preparation, carbonic anhydrase enzyme inhibition and antioxidant activity of novel 7-amino-3,4-dihydroquinolin-2(1H)-one derivatives incorporating mono or dipeptide moiety

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dc.authoridKUCUKBAY, HASAN/0000-0002-7180-9486
dc.authoridGonul, Zeynep/0000-0003-4871-4267
dc.authoridReis, AlessanRSS/0000-0001-8486-7469
dc.authoridangeli, andrea/0000-0002-1470-7192
dc.authoridKucukbay, Fatumetuzzehra/0000-0001-7784-4138
dc.authoridSupuran, Claudiu/0000-0003-4262-0323
dc.authoridBartolucci, Gianluca/0000-0002-5631-8769
dc.authorwosidKUCUKBAY, HASAN/A-5050-2019
dc.contributor.authorKucukbay, Hasan
dc.contributor.authorGonul, Zeynep
dc.contributor.authorKucukbay, F. Zehra
dc.contributor.authorAngeli, Andrea
dc.contributor.authorBartolucci, Gianluca
dc.contributor.authorSupuran, Claudiu T.
dc.date.accessioned2024-08-04T20:47:14Z
dc.date.available2024-08-04T20:47:14Z
dc.date.issued2020
dc.departmentİnönü Üniversitesien_US
dc.description.abstractNew dipeptide-dihydroquinolinone derivatives were successfully synthesised by benzotriazole mediated nucleophilic acyl substitution reaction and their structures were elucidated by spectroscopic and analytic techniques. The carbonic anhydrase (CA, EC 4.2.1.1) inhibitory activity of the new compounds was determined against four human (h) isoforms, hCA I, hCA II, hCA IX and hCA XII. While all compounds showed moderate to good in vitro CA inhibitory properties against hCA IX and hCA XII with inhibition constants in the micromolar level (37.7-86.8 and 2.0-8.6 mu M, respectively), they did not show inhibitory activity against hCA I and hCA II up to 100 mu M concentration. The antioxidant capacity of the peptide-dihydroquinolinone conjugates was determined using 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging method. Most of the synthesised compounds showed low antioxidant activities compared to the control antioxidant compounds BHA and alpha-tocopherol.en_US
dc.description.sponsorshipInonu University, Turkey [BAPB] [FYL-2018-909]; Universita degli Studi di Firenze, Italy; Italian Ministry for University and Research, MIUR [PRIN: rot. 2017XYBP2R]en_US
dc.description.sponsorshipThe authors thank Inonu University, Turkey [BAPB - Grand No. FYL-2018-909], Universita degli Studi di Firenze, Italy and the Italian Ministry for University and Research, MIUR for a grant to CTS [PRIN: rot. 2017XYBP2R].en_US
dc.identifier.doi10.1080/14756366.2020.1751620
dc.identifier.endpage1026en_US
dc.identifier.issn1475-6366
dc.identifier.issn1475-6374
dc.identifier.issue1en_US
dc.identifier.pmid32297533en_US
dc.identifier.scopus2-s2.0-85083477077en_US
dc.identifier.scopusqualityQ1en_US
dc.identifier.startpage1021en_US
dc.identifier.urihttps://doi.org/10.1080/14756366.2020.1751620
dc.identifier.urihttps://hdl.handle.net/11616/99252
dc.identifier.volume35en_US
dc.identifier.wosWOS:000526791200001en_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.subjectDipeptideen_US
dc.subjectdihydroquinolinone derivativesen_US
dc.subjectcarbonic anhydraseen_US
dc.subjectantioxidanten_US
dc.titlePreparation, carbonic anhydrase enzyme inhibition and antioxidant activity of novel 7-amino-3,4-dihydroquinolin-2(1H)-one derivatives incorporating mono or dipeptide moietyen_US
dc.typeArticleen_US

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