Synthesis and carbonic anhydrase inhibitory properties of novel 4-(2-aminoethyl)benzenesulfonamide-dipeptide conjugates

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dc.authoridKUCUKBAY, HASAN/0000-0002-7180-9486
dc.authoridBerrino, Emanuela/0000-0002-4258-0678
dc.authoridSupuran, Claudiu/0000-0003-4262-0323
dc.authoridCAPASSO, CLEMENTE/0000-0003-3314-2411
dc.authoridKucukbay, Fatumetuzzehra/0000-0001-7784-4138
dc.authoridBugday, Nesrin/0000-0002-3882-035X
dc.authoridBartolucci, Gianluca/0000-0002-5631-8769
dc.authorwosidKUCUKBAY, HASAN/A-5050-2019
dc.authorwosidkucukbay, fatumetuzzehra/X-5743-2019
dc.authorwosidBerrino, Emanuela/HJZ-3760-2023
dc.authorwosidCAPASSO, CLEMENTE/P-3522-2016
dc.contributor.authorKucukbay, Hasan
dc.contributor.authorBugday, Nesrin
dc.contributor.authorKucukbay, F. Zehra
dc.contributor.authorBerrino, Emanuela
dc.contributor.authorBartolucci, Gianluca
dc.contributor.authorDel Prete, Sonia
dc.contributor.authorCapasso, Clemente
dc.date.accessioned2024-08-04T20:45:31Z
dc.date.available2024-08-04T20:45:31Z
dc.date.issued2019
dc.departmentİnönü Üniversitesien_US
dc.description.abstractThirty 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.en_US
dc.description.sponsorshipTUBITAK (The Scientific and Technological Research Council of Turkey) [117Z293]; Inonu University, Turkey (BAPB) [FUA-2018-1101]; Universita' degli Studi di Firenze, Italy; European Union of the 7th Framework Program Dynanoen_US
dc.description.sponsorshipWe thank TUBITAK (The Scientific and Technological Research Council of Turkey) Grant No: 117Z293, Inonu University, Turkey (BAPB-Grand No FUA-2018-1101), Universita' degli Studi di Firenze, Italy, and the European Union of the 7th Framework Program Dynano for financial support.en_US
dc.identifier.doi10.1016/j.bioorg.2018.11.003
dc.identifier.endpage423en_US
dc.identifier.issn0045-2068
dc.identifier.issn1090-2120
dc.identifier.pmid30419497en_US
dc.identifier.scopus2-s2.0-85056236913en_US
dc.identifier.scopusqualityQ1en_US
dc.identifier.startpage414en_US
dc.identifier.urihttps://doi.org/10.1016/j.bioorg.2018.11.003
dc.identifier.urihttps://hdl.handle.net/11616/98530
dc.identifier.volume83en_US
dc.identifier.wosWOS:000458609100042en_US
dc.identifier.wosqualityQ1en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.language.isoenen_US
dc.publisherAcademic Press Inc Elsevier Scienceen_US
dc.relation.ispartofBioorganic Chemistryen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectCarbonic anhydraseen_US
dc.subjectInhibitoren_US
dc.subjectSulfonamideen_US
dc.subjectDipeptideen_US
dc.subjectConjugateen_US
dc.titleSynthesis and carbonic anhydrase inhibitory properties of novel 4-(2-aminoethyl)benzenesulfonamide-dipeptide conjugatesen_US
dc.typeArticleen_US

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