Synthesis of novel dipeptide sulfonamide conjugates with effective carbonic anhydrase I, II, IX, and XII inhibitory properties

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dc.authoridKUCUKBAY, HASAN/0000-0002-7180-9486
dc.authoridKazaks, Andris/0000-0003-4964-0984
dc.authoridBartolucci, Gianluca/0000-0002-5631-8769
dc.authoridBugday, Nesrin/0000-0002-3882-035X
dc.authoridSupuran, Claudiu/0000-0003-4262-0323
dc.authoridLeitans, Janis/0000-0002-4853-8147
dc.authoridBua, Silvia/0000-0003-0107-2682
dc.authorwosidKUCUKBAY, HASAN/A-5050-2019
dc.authorwosidKazaks, Andris/AAI-2282-2021
dc.authorwosidLeitans, Janis/AAI-1209-2021
dc.authorwosidkucukbay, fatumetuzzehra/X-5743-2019
dc.contributor.authorBugday, Nesrin
dc.contributor.authorKucukbay, F. Zehra
dc.contributor.authorKucukbay, Hasan
dc.contributor.authorBua, Silvia
dc.contributor.authorBartolucci, Gianluca
dc.contributor.authorLeitans, Janis
dc.contributor.authorKazaks, Andris
dc.date.accessioned2024-08-04T20:45:23Z
dc.date.available2024-08-04T20:45:23Z
dc.date.issued2018
dc.departmentİnönü Üniversitesien_US
dc.description.abstractTwenty-four novel sulfonamide derivatives incorporating dipeptide tails were synthesized by facile acylation reactions of homosulfanilamide through benzotriazole or dicyclohexyl carbodiimide (DCC) mediated coupling reactions. 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 IX and hCA XII. Most of the synthesized compounds showed good in vitro carbonic anhydrase inhibitory properties, with inhibition constants in the low nanomolar range. Particularly, the new dipeptide-sulfonamide conjugates incorporating Ala, Phe and met in the dipeptide sequence, showed the most effective inhibitory activity against to CA IX and XII.en_US
dc.description.sponsorshipTUBITAK (The Scientific and Technological Research Council of Turkey) [117Z293]; Inonu University, Turkey [FUA-2018-1106, FDP-2018-1352]; 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-2018-1106 and FDP-2018-1352), 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.2018.08.032
dc.identifier.endpage318en_US
dc.identifier.issn0045-2068
dc.identifier.issn1090-2120
dc.identifier.pmid30176570en_US
dc.identifier.scopus2-s2.0-85052661729en_US
dc.identifier.scopusqualityQ1en_US
dc.identifier.startpage311en_US
dc.identifier.urihttps://doi.org/10.1016/j.bioorg.2018.08.032
dc.identifier.urihttps://hdl.handle.net/11616/98451
dc.identifier.volume81en_US
dc.identifier.wosWOS:000449428400033en_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.subjectHomosulfanilamideen_US
dc.subjectDipeptideen_US
dc.subjectConjugateen_US
dc.titleSynthesis of novel dipeptide sulfonamide conjugates with effective carbonic anhydrase I, II, IX, and XII inhibitory propertiesen_US
dc.typeArticleen_US

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