Carbonic anhydrase inhibitors: Synthesis, characterization and inhibition activities of furan sulfonylhydrazones against carbonic anhydrase I (hCA I)

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dc.contributor.authorBalaban Gündüzalp, Ayla
dc.contributor.authorParlakgümüş, Gökhan
dc.contributor.authorUzun, Demet
dc.contributor.authorÖzmen, Ümmühan Özdemir
dc.contributor.authorÖzbek, Neslihan
dc.contributor.authorSarı, Musa
dc.contributor.authorTunç, Tuncay
dc.date.accessioned13.07.201910:50:10
dc.date.accessioned2019-07-29T19:27:34Z
dc.date.available13.07.201910:50:10
dc.date.available2019-07-29T19:27:34Z
dc.date.issued2016
dc.departmentEğitim Fakültesi
dc.description.abstractThe methane sulfonic acide hydrazide (1) was used to obtain furan sulfonylhydrazones; 2acetylfuranmethanesulfonylhydrazone (2), 2-furaldehydemethanesulfonylhydrazone (3), 5-nitro-2furaldehydemethanesulfonylhydrazone (4). The structures of furan sulfonylhydrazones were determined by using elemental analysis, FT-IR, H-1 NMR, C-13 NMR and UV vis methods. The structure of 5nitro-2-furaldehydemethanesulfonylhydrazone (4) was also supported with X-ray difraction method and found that compound 4 was crystallized in triclinic, space group PT. In order to gain insight into the structure of the compounds, we performed computational studies by using 6-311G(d,p) basic set in which B3LYP correlation function was implemented. The geometry of the sulfonylhydrazones were optimized at DFT method with Gaussian 09 program package and the global reactivity descriptors were also calculated by this basic set. The enzyme inhibition activities of the sulfonylhydrazones were investigated on carbonic anhydrase I (hCA I) isoenzyme and their activity parameters (Km, IC50 and Ki) were calculated by spectrophotometric method. And also, their inhibitor effects were also investigated by cyclic voltammetry (CV) and differential pulse voltammetry (DPV) methods. Inhibition results show that compound 4 containing electron withdrawing group (NO2) has higher inhibition effect on hCA I isoenzyme than other's.
dc.description.sponsorshipGazi University Research Found [05/2011-27]; Aksaray University Science and Technology Application and Research Center (of the State of Planning Organization) [2010K120480]
dc.description.sponsorshipThis research was funded by Gazi University Research Found under Project No 05/2011-27. We are thankful to Aksaray University Science and Technology Application and Research Center, for the use of the Bruker SMART BREEZE CCD diffractometer (purchased under grant No. 2010K120480 of the State of Planning Organization). I'm thankful to my mother (Gulsahin Balaban, died in July 13, 2014) for her support in my life.
dc.identifier.doi10.1016/j.molstruc.2015.10.054
dc.identifier.endpage340en_US
dc.identifier.issn0022-2860
dc.identifier.issn1872-8014
dc.identifier.scopusqualityQ1
dc.identifier.startpage332en_US
dc.identifier.urihttps://doi.org/10.1016/j.molstruc.2015.10.054
dc.identifier.urihttps://hdl.handle.net/20.500.12451/5890
dc.identifier.volume1105en_US
dc.identifier.wosWOS:000366238100040
dc.identifier.wosqualityN/A
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.language.isoen
dc.publisherElsevier Science Bv
dc.relation.ispartofJournal of Molecular Structure
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/closedAccess
dc.subjectCarbonic Anhydrase I (hCA I)
dc.subjectEnzyme Inhibition
dc.subjectFuran Sulfonylhydrazone
dc.subjectCyclic Voltammetty (CV)
dc.subjectDifferantial Pulse Voltammetry (DPV)
dc.titleCarbonic anhydrase inhibitors: Synthesis, characterization and inhibition activities of furan sulfonylhydrazones against carbonic anhydrase I (hCA I)
dc.typeArticle

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