Synthesis, characterization, crystal structures, theoretical calculations and biological evaluations of novel substituted tacrine derivatives as cholinesterase and carbonic anhydrase enzymes inhibitors

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dc.contributor.authorOkten, Salih
dc.contributor.authorEkiz, Makbule
dc.contributor.authorKocyigit, Umit Muhammet
dc.contributor.authorTutar, Ahmet
dc.contributor.authorCelik, Ismail
dc.contributor.authorAkkurt, Mehmet
dc.contributor.authorGulcin, Ilhami
dc.date.accessioned2020-06-25T18:34:22Z
dc.date.available2020-06-25T18:34:22Z
dc.date.issued2019
dc.departmentKırıkkale Üniversitesi
dc.descriptionOkten, Salih/0000-0001-9656-1803; GULCIN, Ilhami/0000-0001-5993-1668;
dc.description.abstractThe six and seven hydrocycle membered disilylanilino acridine (tacrine) analogues (9-11) were synthesized by one-pot procedures. The structures of novel silyl tacrine derivatives were characterized by NMR spectroscopy, elemental analysis and XRD investigations. The silyl substituted novel tacrine derivatives (9-11) were investigated as cholinesterase inhibitors and defined the relative role of AChE (Acetylcholinesterase) versus BChE (Butyrylcholinesterase) inhibition. Novel substituted tacrine derivatives are known as important inhibitors of Carbonic anhydrase (CA) isoenzymes I, and II (hCA I and II), therefore, the synthesized compounds (9-11) were investigated for inhibitory effects on the both CA isoenzymes. Additionally, we evaluated four different enzymes, which were inhibited in the very low nanomolar (nM) range by these compounds. According to the present studies, for AChE, BChE, hCA I and II, the ranges of results are recorded as 30.26 +/- 6.71-117.54 +/- 42.22 nM, 22.45 +/- 5.81-77.41 +/- 4.02 nM, 57.28 +/- 22.16-213.41 +/- 82.75 nM and 46.95 +/- 11.32-274.94 +/- 62.15 nM, respectively. (C) 2018 Elsevier B.V. All rights reserved.en_US
dc.identifier.citationclosedAccessen_US
dc.identifier.doi10.1016/j.molstruc.2018.08.063
dc.identifier.endpage915en_US
dc.identifier.issn0022-2860
dc.identifier.issn1872-8014
dc.identifier.scopus2-s2.0-85052137357
dc.identifier.scopusqualityQ1
dc.identifier.startpage906en_US
dc.identifier.urihttps://doi.org/10.1016/j.molstruc.2018.08.063
dc.identifier.urihttps://hdl.handle.net/20.500.12587/7884
dc.identifier.volume1175en_US
dc.identifier.wosWOS:000449141100096
dc.identifier.wosqualityQ3
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.language.isoen
dc.publisherElsevier Science Bven_US
dc.relation.ispartofJournal Of Molecular Structure
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectSilyl tacrineen_US
dc.subjectDeprotonation of amineen_US
dc.subjectAcetylcholinesteraseen_US
dc.subjectButyrylcholinesteraseen_US
dc.subjectCarbonic anhydraseen_US
dc.subjectEnzyme inhibitoren_US
dc.titleSynthesis, characterization, crystal structures, theoretical calculations and biological evaluations of novel substituted tacrine derivatives as cholinesterase and carbonic anhydrase enzymes inhibitorsen_US
dc.typeArticle

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