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N-Acylsulfonamides strongly inhibit human carbonic anhydrase isoenzymes i and II

MakaleAçık Erişim

Özet

Sulfonamides represent a significant class of biologically active compounds that inhibit carbonic anhydrase (CA, EC.: 4.2.1.1) isoenzymes involved in different pathological and physiological events. Sulfonamide CA inhibitors are used therapeutically as diuretic, antiglaucoma, antiobesity and anticancer agents. A series of new sulfonamides were synthesized using imides and tosyl chloride as starting materials. These N-acylsulfonamides efficiently inhibited the cytosolic human carbonic anhydrase isoenzymes I, and II (hCA I, and II), with nanomolar range inhibition constants ranging between 36.4 ± 6.0-254.6 ± 18.0 and 58.3 ± 0.6-273.3 ± 2.5 nM, respectively.

Anahtar Kelimeler

Carbonic anhydraseEnzyme inhibitionEnzyme purificationImideN-AcylsulfonamideSulfonamide
RDL Kalıcı Bağlantı (PID)
https://rdlopen.rawdatalibrary.net/r/gumushane/15391Resmi atıflarda kullanılan kalıcı adres
DOI
https://doi.org/10.1016/j.bmc.2014.12.054Yayıncı resmi DOI adresi
Tam Kayıt
AlanDeğerDil
dc.contributor.authorYildirim, Alper
dc.contributor.authorAtmaca, Ufuk
dc.contributor.authorKeskin, Ali
dc.contributor.authorTopal, Meryem
dc.contributor.authorÇelik, Murat
dc.contributor.authorGülçin, Ilhami
dc.contributor.authorSupuran, Claudiu T.
dc.date.accessioned2026-10-22T10:23:57.226961753Z
dc.date.available2026-10-22T10:23:57.226961753Z
dc.date.issued2015
dc.description.abstractSulfonamides represent a significant class of biologically active compounds that inhibit carbonic anhydrase (CA, EC.: 4.2.1.1) isoenzymes involved in different pathological and physiological events. Sulfonamide CA inhibitors are used therapeutically as diuretic, antiglaucoma, antiobesity and anticancer agents. A series of new sulfonamides were synthesized using imides and tosyl chloride as starting materials. These N-acylsulfonamides efficiently inhibited the cytosolic human carbonic anhydrase isoenzymes I, and II (hCA I, and II), with nanomolar range inhibition constants ranging between 36.4 ± 6.0-254.6 ± 18.0 and 58.3 ± 0.6-273.3 ± 2.5 nM, respectively.
dc.description.sponsorshipAtaturk University
dc.description.sponsorshipTUBITAK, (110T483)
dc.description.sponsorshipKing Saud University, KSU
dc.identifier.doi10.1016/j.bmc.2014.12.054
dc.identifier.eissn1464-3391
dc.identifier.endpage2605
dc.identifier.issn0968-0896
dc.identifier.issue10
dc.identifier.pmid25863492
dc.identifier.scopus2-s2.0-84937765332
dc.identifier.startpage2598
dc.identifier.urihttps://rdlopen.rawdatalibrary.net/r/gumushane/15391
dc.identifier.volume23
dc.identifier.wosWOS:000353380400029
dc.language.isoen
dc.publisherElsevier Ltd
dc.relation.ispartofBioorganic and Medicinal Chemistry
dc.rightsinfo:eu-repo/semantics/openAccess
dc.subjectCarbonic anhydrase
dc.subjectEnzyme inhibition
dc.subjectEnzyme purification
dc.subjectImide
dc.subjectN-Acylsulfonamide
dc.subjectSulfonamide
dc.subject.classificationBiochemistry & Molecular Biology
dc.subject.classificationChemistry, Medicinal
dc.subject.classificationChemistry, Organic
dc.subject.classificationPharmacology & Pharmacy
dc.subject.classificationChemistry
dc.subject.otherCarbonic Anhydrase I
dc.subject.otherCarbonic Anhydrase II
dc.subject.otherCarbonic Anhydrase Inhibitors
dc.subject.otherHumans
dc.subject.otherImides
dc.subject.otherKinetics
dc.subject.otherMolecular Structure
dc.subject.otherStructure-Activity Relationship
dc.subject.otherSulfonamides
dc.subject.otherTosyl Compounds
dc.subject.other4-toluenesulfonyl chloride
dc.subject.othercarbonate dehydratase I
dc.subject.othercarbonate dehydratase II
dc.subject.othercarbonate dehydratase inhibitor
dc.subject.otherimide
dc.subject.othersulfonamide
dc.subject.othertoluenesulfonic acid derivative
dc.subject.otherantagonists and inhibitors
dc.subject.otherchemical structure
dc.subject.otherchemistry
dc.subject.otherhuman
dc.subject.otherstructure activity relation
dc.subject.othersynthesis
dc.titleN-Acylsulfonamides strongly inhibit human carbonic anhydrase isoenzymes i and II
dc.typeArticle
dspace.entity.typePublication
rdl.citation.scopus158
rdl.citation.wos155
rdl.departmentGumushane University, Vocational School of Health Services, Department of Medical Services and Techniques, Gumushane, Turkey
rdl.oa.statusgreen
rdl.oa.statusclosed
rdl.oa.urlhttps://doi.org/10.7270/q2959k7q
rdl.source.indexSCOPUS
rdl.source.indexWOS
rdl.source.indexPUBMED
rdl.wos.indexScience Citation Index Expanded (SCI-EXPANDED)
rdl.wos.indexIndex Chemicus (IC)