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Some N-(5-methyl-1,3,4-thiadiazol-2-yl)-4-[(3-substituted)ureido/thioureido]benzenesulfonamides as carbonic anhydrase I and II Inhibitors

dc.contributor.authorKAYMAKÇIOĞLU, BEDİA
dc.contributor.authorsTurk, Sevda; Tok, Fatih; Celik, Hulya; Karakus, Sevgi; Nadaroglu, Hayrunnisa; Kocyigit-Kaymakcioglu, Bedia; Kucukoglu, Kaan
dc.date.accessioned2022-03-14T08:27:18Z
dc.date.available2022-03-14T08:27:18Z
dc.date.issued2016-08-25
dc.description.abstractIn the present study, N-(5-methyl-1,3,4-thiadiazol-2-yl)-4-[(3-substituted)ureido]benzenesulfonamide (1-9) and N-(5-methyl-1,3,4-thiadiazol-2-yl)-4-[(3-substituted) thioureido]benzenesulfonamide (10-14) derivatives were synthesized from 4-amino-N-(5-methyl-1,3,4-thiadiazol-2-yl) benzenesulfonamide (sulfamethizole). All new compounds were characterized by elemental analysis and various spectroscopic methods (FTIR, H-1-NMR and MS). These new sulfonamide derivatives were investigated as inhibitors of carbonic anhydrase especially human carbonic anhydrase I and II. The new compounds showed higher activity against the human cytosolic CA I (IC50 values 0.144-15.65 nM) and CA II (IC50 values 0.109-17.95 nM) in comparison with the clinically used CA inhibitor acetazolamide.
dc.identifier.doi10.12991/marupj.259885
dc.identifier.issn1309-0801
dc.identifier.urihttps://hdl.handle.net/11424/241811
dc.identifier.wosWOS:000391177500011
dc.language.isoeng
dc.publisherMARMARA UNIV, FAC PHARMACY
dc.relation.ispartofMARMARA PHARMACEUTICAL JOURNAL
dc.rightsinfo:eu-repo/semantics/openAccess
dc.subjectCarbonic anhydrase inhibitors
dc.subjectsulfonamide
dc.subjectsulfamethizole
dc.subjecturea and thiourea
dc.subjectPURIFICATION
dc.subjectXII
dc.titleSome N-(5-methyl-1,3,4-thiadiazol-2-yl)-4-[(3-substituted)ureido/thioureido]benzenesulfonamides as carbonic anhydrase I and II Inhibitors
dc.typearticle
dspace.entity.typePublication
local.avesis.ida2a6ad12-5c2a-4a37-8e32-dce27fb54ad9
local.import.packageSS16
local.indexed.atWOS
local.indexed.atSCOPUS
local.journal.numberofpages7
oaire.citation.endPage95
oaire.citation.issue1
oaire.citation.startPage89
oaire.citation.titleMARMARA PHARMACEUTICAL JOURNAL
oaire.citation.volume21
relation.isAuthorOfPublication0f8e7ba6-02e7-4232-84bb-31777a356761
relation.isAuthorOfPublication.latestForDiscovery0f8e7ba6-02e7-4232-84bb-31777a356761

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