Novel NHC Precursors: Synthesis, Characterization, and Carbonic Anhydrase and Acetylcholinesterase Inhibitory Properties

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dc.authoridGulcin, ilhami/0000-0001-5993-1668
dc.authoridAktaş, Aydın/0000-0001-8496-6782
dc.authoridTaslimi, Parham/0000-0002-3171-0633
dc.authorwosidGulcin, ilhami/F-1428-2014
dc.authorwosidTaslimi, Parham/AAL-2788-2020
dc.authorwosidGök, Yetkin/AAA-5669-2021
dc.authorwosidAktaş, Aydın/J-6194-2019
dc.contributor.authorAktas, Aydin
dc.contributor.authorTaslimi, Parham
dc.contributor.authorGulcin, Ilhami
dc.contributor.authorGok, Yetkin
dc.date.accessioned2024-08-04T20:43:09Z
dc.date.available2024-08-04T20:43:09Z
dc.date.issued2017
dc.departmentİnönü Üniversitesien_US
dc.description.abstractThree series of imidazolidinium ligands (NHC precursors) substituted with 4-vinylbenzyl, 2-methyl-1,4-benzodioxane, and N-propylphthalimide were synthesized. N-Heterocyclic carbene (NHC) precursors were prepared from N-alkylimidazoline and alkyl halides. The novel NHC precursors were characterized by H-1 NMR, C-13 NMR, FTIR spectroscopy, and elemental analysis techniques. The enzymes inhibition activities of the NHC precursors were investigated against the cytosolic human carbonic anhydrase I and II isoenzymes (hCA I and II) and the acetylcholinesterase (AChE) enzyme. The inhibition parameters (IC50 and K-i values) were calculated by spectrophotometric method. The inhibition constants (K-i) were found to be in the range of 166.65-635.38nM for hCA I, 78.79-246.17nM for hCA II, and 23.42-62.04nM for AChE. Also, the inhibitory effects of the novel synthesized NHCs were compared to acetazolamide as a clinical CA isoenzymes inhibitor and tacrine as a clinical cholinergic enzymes inhibitor.en_US
dc.description.sponsorshipInonu University, Research Project Unit [2011/25]en_US
dc.description.sponsorshipThe financial support was provided by Inonu University, Research Project Unit (Project No: 2011/25).en_US
dc.identifier.doi10.1002/ardp.201700045
dc.identifier.issn0365-6233
dc.identifier.issn1521-4184
dc.identifier.issue6en_US
dc.identifier.pmid28464340en_US
dc.identifier.scopus2-s2.0-85018963565en_US
dc.identifier.scopusqualityQ2en_US
dc.identifier.urihttps://doi.org/10.1002/ardp.201700045
dc.identifier.urihttps://hdl.handle.net/11616/97805
dc.identifier.volume350en_US
dc.identifier.wosWOS:000402923500005en_US
dc.identifier.wosqualityQ2en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.language.isoenen_US
dc.publisherWiley-V C H Verlag Gmbhen_US
dc.relation.ispartofArchiv Der Pharmazieen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectAcetylcholinesteraseen_US
dc.subjectCarbonic anhydraseen_US
dc.subjectEnzyme inhibitionen_US
dc.subjectEnzyme purificationen_US
dc.subjectN-Heterocyclic carbenesen_US
dc.titleNovel NHC Precursors: Synthesis, Characterization, and Carbonic Anhydrase and Acetylcholinesterase Inhibitory Propertiesen_US
dc.typeArticleen_US

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