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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.author Ökten, Salih
dc.contributor.author Ekiz, Makbule
dc.contributor.author Koçyiğit, Ümit Muhammet
dc.contributor.author Tutar, Ahmet
dc.contributor.author Çelik, İsmail
dc.contributor.author Akkurt, Mehmet
dc.contributor.author Gökalp, Faik
dc.contributor.author Taslimi, Parham
dc.contributor.author Gülçin, İlhami
dc.date.accessioned 2019-04-29T08:39:20Z
dc.date.available 2019-04-29T08:39:20Z
dc.date.issued 2019-01-05
dc.identifier.uri http://hdl.handle.net/11772/1132
dc.description.abstract The 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.language.iso eng en_US
dc.publisher Elsevier en_US
dc.relation.isversionof 10.1016/j.molstruc.2018.08.063 en_US
dc.rights info:eu-repo/semantics/restrictedAccess en_US
dc.subject Silyl tacrine en_US
dc.subject Deprotonation of amine en_US
dc.subject Acetylcholinesterase en_US
dc.subject Butyrylcholinesterase en_US
dc.subject Carbonic anhydrase en_US
dc.subject Enzyme inhibitor en_US
dc.title Synthesis, characterization, crystal structures, theoretical calculations and biological evaluations of novel substituted tacrine derivatives as cholinesterase and carbonic anhydrase enzymes inhibitors en_US
dc.type article en_US
dc.relation.journal Journal Of Molecular Structure en_US
dc.contributor.department Bartın Üniversitesi, Fen Fakültesi, Biyoteknoloji Bölümü en_US
dc.identifier.volume 1175 en_US
dc.identifier.startpage 906 en_US
dc.identifier.endpage 915 en_US


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