dc.contributor.author | Okten, Salih | |
dc.contributor.author | Ekiz, Makbule | |
dc.contributor.author | Kocyigit, Umit Muhammet | |
dc.contributor.author | Tutar, Ahmet | |
dc.contributor.author | Celik, Ismail | |
dc.contributor.author | Akkurt, Mehmet | |
dc.contributor.author | Gokalp, Faik | |
dc.contributor.author | Taslimi, Parham | |
dc.contributor.author | Gulcin, Ilhami | |
dc.date.accessioned | 2019-07-27T12:10:23Z | |
dc.date.accessioned | 2019-07-28T09:37:15Z | |
dc.date.available | 2019-07-27T12:10:23Z | |
dc.date.available | 2019-07-28T09:37:15Z | |
dc.date.issued | 2019 | |
dc.identifier.issn | 0022-2860 | |
dc.identifier.issn | 1872-8014 | |
dc.identifier.uri | https://dx.doi.org/10.1016/j.molstruc.2018.08.063 | |
dc.identifier.uri | https://hdl.handle.net/20.500.12418/5993 | |
dc.description | WOS: 000449141100096 | en_US |
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 SCIENCE BV | en_US |
dc.relation.isversionof | 10.1016/j.molstruc.2018.08.063 | en_US |
dc.rights | info:eu-repo/semantics/closedAccess | 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 | [Okten, Salih -- Gokalp, Faik] Kirikkale Univ, Fac Educ, Dept Maths & Sci Educ, TR-71450 Yahsihan, Kirikkale, Turkey -- [Ekiz, Makbule -- Tutar, Ahmet] Sakarya Univ, Fac Art & Sci, Dept Chem, TR-54187 Serdivan, Sakarya, Turkey -- [Kocyigit, Umit Muhammet] Cumhuriyet Univ, Vocat Sch Hlth Serv, TR-58140 Sivas, Turkey -- [Celik, Ismail] Cumhuriyet Univ, Fac Sci, Dept Phys, TR-58140 Sivas, Turkey -- [Akkurt, Mehmet] Erciyes Univ, Fac Sci, Dept Phys, TR-38039 Kayseri, Turkey -- [Taslimi, Parham -- Gulcin, Ilhami] Ataturk Univ, Fac Sci, Dept Chem, TR-25240 Erzurum, Turkey | en_US |
dc.contributor.authorID | Okten, Salih -- 0000-0001-9656-1803 | en_US |
dc.identifier.volume | 1175 | en_US |
dc.identifier.endpage | 915 | en_US |
dc.identifier.startpage | 906 | en_US |
dc.relation.publicationcategory | Makale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı | en_US |