Synthesis carbonic anhydrase enzyme inhibition and antioxidant activity of novel benzothiazole derivatives incorporating glycine, methionine, 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.authoridangeli, andrea/0000-0002-1470-7192
dc.authorwosidkucukbay, fatumetuzzehra/X-5743-2019
dc.authorwosidKUCUKBAY, HASAN/A-5050-2019
dc.contributor.authorPayaz, Deniz Uzeroglu
dc.contributor.authorKucukbay, F. Zehra
dc.contributor.authorKucukbay, Hasan
dc.contributor.authorAngeli, Andrea
dc.contributor.authorSupuran, Claudiu T.
dc.date.accessioned2024-08-04T20:45:37Z
dc.date.available2024-08-04T20:45:37Z
dc.date.issued2019
dc.departmentİnönü Üniversitesien_US
dc.description.abstractThirteen novel benzothiazole derivatives incorporating glycine, methionine, alanine, and phenylalanine were synthesised by facile acylation reactions through benzotriazole or DCC mediated reactions and their structures were identified by H-1-NMR, 13C-NMR, 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 V, and hCA XIII. Some of the synthesised compounds showed good in vitro carbonic anhydrase inhibitory properties, with inhibition constants in the micromolar level. The new amino acid benzothiazole conjugates found to be more effective against hCA V and hCA II inhibition. In vitro antioxidant activities of the novel compounds were determined by DPPH method. Most of the synthesised compounds showed moderate to low antioxidant activities compared to the control antioxidant compounds (BHA and alpha-tocopherol).en_US
dc.description.sponsorshipInonu University, Turkey (BAPB) [2016/94]; Universita degli Studi di Firenze, Italyen_US
dc.description.sponsorshipWe thank Inonu University, Turkey (BAPB - Grand No-2016/94) and Universita degli Studi di Firenze, Italy.en_US
dc.identifier.doi10.1080/14756366.2018.1553040
dc.identifier.endpage349en_US
dc.identifier.issn1475-6366
dc.identifier.issn1475-6374
dc.identifier.issue1en_US
dc.identifier.pmid30734592en_US
dc.identifier.scopus2-s2.0-85059199925en_US
dc.identifier.scopusqualityQ1en_US
dc.identifier.startpage343en_US
dc.identifier.urihttps://doi.org/10.1080/14756366.2018.1553040
dc.identifier.urihttps://hdl.handle.net/11616/98588
dc.identifier.volume34en_US
dc.identifier.wosWOS:000454390900001en_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.subjectBenzothiazoleen_US
dc.subjectamino acidsen_US
dc.subjectcarbonic anhydraseen_US
dc.subjectantioxidanten_US
dc.subjectbenzotriazole methodologyen_US
dc.titleSynthesis carbonic anhydrase enzyme inhibition and antioxidant activity of novel benzothiazole derivatives incorporating glycine, methionine, alanine, and phenylalanine moietiesen_US
dc.typeArticleen_US

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