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Synthesis, antioxidant and carbonic anhydrase I and II inhibitory activities of novel sulphonamide-substituted coumarylthiazole derivatives

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dc.contributor.authorKurt, BELMA
dc.contributor.authorSonmez, Fatih
dc.contributor.authorBilen, Cigdem
dc.contributor.authorErgun, Adem
dc.contributor.authorGencer, Nahit
dc.contributor.authorArslan, Oktay
dc.contributor.authorKucukislamoglu, Mustafa
dc.contributor.institutionauthorZENGİN KURT, BELMA
dc.date.accessioned2019-10-05T21:33:38Z
dc.date.available2019-10-05T21:33:38Z
dc.date.issued2016-01-01
dc.description.abstractNew secondary benzenesulphonamide-substituted coumarylthiazole derivatives were synthesized and their inhibitory effects on purified carbonic anhydrase I and II were evaluated using CO2 as a substrate. The result showed that all the synthesized compounds exhibited inhibitory activity on both hCA I and hCA II with N-(4-(2-oxo-2H-chromen-3-yl)thiazol-2-yl) naphthalene-2-sulphonamide (5f, IC50 value of 5.63 and 8.48 mu M, against hCA I and hCA II, respectively) as the strongest inhibitor revealed from this study. Structure-activity relationship revealed that the inhibitory activity of the synthesized compounds is related to the type of the halogen and bulky substituent on the phenyl ring. In addition, the cupric reducing antioxidant capacities (CUPRAC) and ABTS cation radical scavenging abilities of the synthesized compounds were assayed. 4-methoxy-N-(4-(2-oxo-2H-chromen-3-yl) thiazol-2-yl) benzenesulphonamide (5e) exhibited the strongest ABTS and CUPRAC activity with IC50 value of 48.83 mu M and A(0.50) value of 23.29 mu M ,
dc.identifier
dc.identifier.citationKurt B., Sonmez F., Bilen C., Ergun A., Gencer N., Arslan O., Kucukislamoglu M., -Synthesis, antioxidant and carbonic anhydrase I and II inhibitory activities of novel sulphonamide-substituted coumarylthiazole derivatives-, JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, cilt.31, ss.991-998, 2016
dc.identifier.pubmed26309156
dc.identifier.urihttps://hdl.handle.net/20.500.12645/7613
dc.language.isoen
dc.titleSynthesis, antioxidant and carbonic anhydrase I and II inhibitory activities of novel sulphonamide-substituted coumarylthiazole derivatives
dc.typeArticle
dspace.entity.typePublication
local.article.journalnameÇOCUK SAĞLIĞI VE HASTALIKLARI DERGİSİ
local.avesis.idbd34e167-a432-44ed-80cc-08111215309b
local.avesis.response7489
relation.isAuthorOfPublication3fd265b5-fdd8-4c56-949b-deb0303c3db7
relation.isAuthorOfPublication.latestForDiscovery3fd265b5-fdd8-4c56-949b-deb0303c3db7
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