The synthesis of novel pyrazole-3,4-dicarboxamidesbearing 5-amino-1,3,4-thiadiazole-2-sulfonamide moiety with effective inhibitory activity against the isoforms of human cytosolic carbonic anhydrase I and II

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dc.authorid0000-0003-3667-6902en_US
dc.contributor.authorMert, Samet
dc.contributor.authorAlim, Zuhal
dc.contributor.authorIsgor, Mehmet Mustafa
dc.contributor.authorBeydemir, Şükrü
dc.contributor.authorKasimogullari, Rahmi
dc.date.accessioned2021-03-20T20:14:24Z
dc.date.available2021-03-20T20:14:24Z
dc.date.issued2016
dc.departmentBTÜ, Mühendislik ve Doğa Bilimleri Fakültesi, Kimya Bölümüen_US
dc.description.abstractA series of 1-(3-substituted-phenyl)-5-phenyl-N-3,N-4-bis(5-sulfamoyl-1,3,4-thiadiazol-2-yl)-1H-pyrazole-3,4- dicarboxamides (4-15) were synthesized. The structures of these pyrazole-sulfonamides were confirmed by FT-IR, H-1 NMR, C-13 NMR and elemental analysis methods. Human cytosolic carbonic anhydrase (CA, EC 4.2.1.1) isozymes (hCA I and II) were purified from erythrocyte cells by affinity chromatography. The inhibitory effects of newly synthesized derivatives (4-15) were investigated in vitro on esterase activities of these isozymes. The K-i values were determined as 0.119-3.999 mu M for hCA I and 0.084-0.878 mu Mfor hCA II. The results showed that the compound 6 for hCA I and the compound 11 for hCA II had the highest inhibitory effect. Beside that, the compound 8 had the lowest inhibition effect on both isozymes. (C) 2016 Elsevier Inc. All rights reserved.en_US
dc.description.sponsorshipDumlupinar University Research FundDumlupinar University [2010/14]en_US
dc.description.sponsorshipThis work was supported by the Dumlupinar University Research Fund (Project Number: 2010/14). Also the authors are grateful to the Ataturk University Faculty of Sciences Department of Chemistry for providing the usage of spectroanalytic laboratory facilities and Dumlupinar University Faculty of Arts and Sciences Department of Physics for FT-IR measurements.en_US
dc.identifier.doi10.1016/j.bioorg.2016.07.006en_US
dc.identifier.endpage71en_US
dc.identifier.issn0045-2068
dc.identifier.issn1090-2120
dc.identifier.pmid27454619en_US
dc.identifier.scopusqualityQ1en_US
dc.identifier.startpage64en_US
dc.identifier.urihttp://doi.org/10.1016/j.bioorg.2016.07.006
dc.identifier.urihttps://hdl.handle.net/20.500.12885/1048
dc.identifier.volume68en_US
dc.identifier.wosWOS:000387978400008en_US
dc.identifier.wosqualityQ2en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.institutionauthorBeydemir, Şükrü
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.subjectPyrazole-3,4-dicarboxylic aciden_US
dc.subject1,3,4-Thiadiazole-2-sulfonamideen_US
dc.subjectSynthesisen_US
dc.subjectAntiglaucomaen_US
dc.subjectInhibitionen_US
dc.subjectCarbonic anhydraseen_US
dc.titleThe synthesis of novel pyrazole-3,4-dicarboxamidesbearing 5-amino-1,3,4-thiadiazole-2-sulfonamide moiety with effective inhibitory activity against the isoforms of human cytosolic carbonic anhydrase I and IIen_US
dc.typeArticleen_US

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