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dc.contributor.authorTopal, Fevzi
dc.contributor.authorGulcin, Ilhami
dc.contributor.authorDastan, Arif
dc.contributor.authorGuney, Murat
dc.date.accessioned2021-11-09T19:49:50Z
dc.date.available2021-11-09T19:49:50Z
dc.date.issued2017
dc.identifier.issn0141-8130
dc.identifier.issn1879-0003
dc.identifier.urihttps://doi.org/10.1016/j.ijbiomac.2016.10.096
dc.identifier.urihttps://hdl.handle.net/20.500.12440/4136
dc.description.abstractEugenol was used as starting material to obtain some phenolic compounds. The synthesis of these phenolic compounds was performed in a two-step procedure. The structures of the formed products (novel eugenol derivatives 1-6) have been determined on the basis of NMR spectroscopy and other spectroscopic methods. The compounds were tested in terms of carbonic anhydrase (CA) inhibition potency. Carbonic anhydrases (CAs, EC 4.2.1.1) are metalloenzymes, which catalyse the reaction between carbon dioxide (CO2) and water (H2O), to generate bicarbonate (HCO3-) and protons (H+). CO2, HCO3- and H+ are essential molecules and ions for many important physiologic processes occurring in all living organisms. Acetylcholinesterase (AChE, E.C.3.1.1.7) is found in high concentrations in the red blood cells and brain. Novel eugenol derivatives (1-6) were tested for the inhibition of two cytosolic CA isoforms 1, and II (hCA I, and II) and AChE. These compounds demonstrated effective inhibitory profiles with Ki values in ranging of 113.48-738.69 nM against hCA I, 92.35-530.81 nM against hCA II, and 90.10-379.57 nM against AChE, respectively. On the other hand, acetazolamide clinically used as CA inhibitor, shoed Ki value of 594.11 nM against hCA I, and 120.68 nM against hCA II, respectively. Also, AChE was inhibited by tacrine as an AChE inhibitor at the 71.18 nM level. (C) 2016 Elsevier B.V. All rights reserved.en_US
dc.language.isoengen_US
dc.publisherElsevier Science Bven_US
dc.relation.ispartofInternational Journal of Biological Macromoleculesen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectEugenolen_US
dc.subjectCarbonic anhydraseen_US
dc.subjectAcetylcholinesteraseen_US
dc.subjectEnzyme purificationen_US
dc.subjectEnzyme inhibitionen_US
dc.titleNovel eugenol derivatives: Potent acetylcholinesterase and carbonic anhydrase inhibitorsen_US
dc.typearticleen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.description.wospublicationidWOS:000390496100014en_US
dc.description.scopuspublicationid2-s2.0-85002002669en_US
dc.departmentGümüşhane Üniversitesien_US
dc.authoridGULCIN, Ilhami / 0000-0001-5993-1668
dc.authoridDastan, Arif / 0000-0002-9577-2251
dc.identifier.volume94en_US
dc.identifier.startpage845en_US
dc.identifier.doi10.1016/j.ijbiomac.2016.10.096
dc.identifier.endpage851en_US
dc.authorwosidGULCIN, Ilhami / F-1428-2014
dc.authorscopusid35811768400
dc.authorscopusid35509141500
dc.authorscopusid6701810213
dc.authorscopusid8527557100
dc.description.pubmedpublicationidPubMed: 27984137en_US


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