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The first synthesis, carbonic anhydrase inhibition and anticholinergic activities of some bromophenol derivatives with S including natural products

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dc.contributor.author Bayrak, Cetin
dc.contributor.author Taslimi, Parham
dc.contributor.author Karaman, Halide Sedef
dc.contributor.author Gulcin, Ilhami
dc.contributor.author Menzek, Abdullah
dc.date.accessioned 2019-04-29T07:48:00Z
dc.date.available 2019-04-29T07:48:00Z
dc.date.issued 2019-04
dc.identifier.uri http://hdl.handle.net/11772/1121
dc.description.abstract Starting from vanillin, known four benzyl bromides with Br were synthesized. The first synthesis of natural product 3,4-dibromo-5-((methylsulfonyl)methyl)benzene-1,2-diol (2) and 3,4,6-tribromo-5-((methylsulfonyl) methyl)benzene-1,2-diol (3) and derivatives were carried out by demethylation, acetylatilation, oxidation and hydrolysis reactions of the benzyl bromides. Also, these compounds were tested against some important enzymes like acetylcholinesterase and butyrylcholinesterase enzymes, carbonic anhydrase I, and II isoenzymes. The novel bromophenols showed Ki values of in range of 53.75 +/- 12.54-234.68 +/- 46.76 nM against hCA I, 42.84 +/- 9.36 and 200.54 +/- 57.25 nM against hCA II, 0.84 +/- 0.12-14.63 +/- 3.06 nM against AChE and 0.93 +/- 0.20-18.53 +/- 5.06 nM against BChE. Induced fit docking process performed on the compounds inhibiting hCA I, hCA II, AChE, and BChE receptors. Hydroxyl group should exist at the aromatic ring of the compounds for inhibition of the enzymes. The moieties reported in this study will be useful for design of more potent and selective inhibitors against the enzymes. en_US
dc.language.iso eng en_US
dc.publisher Bioorganic Chemistry en_US
dc.relation.isversionof 10.1016/j.bioorg.2018.12.012 en_US
dc.rights info:eu-repo/semantics/restrictedAccess en_US
dc.subject Bromination en_US
dc.subject Bromophenol en_US
dc.subject Carbonic anhydrase en_US
dc.subject Acetylcholinesterase en_US
dc.subject Enzyme inhibition en_US
dc.subject Molecular docking en_US
dc.title The first synthesis, carbonic anhydrase inhibition and anticholinergic activities of some bromophenol derivatives with S including natural products en_US
dc.type article en_US
dc.relation.journal Bioorganic Chemistry en_US
dc.contributor.department Bartın Üniversitesi, Fen Fakültesi, Biyoteknoloji Bölümü en_US
dc.identifier.volume 85 en_US
dc.identifier.startpage 128 en_US
dc.identifier.endpage 139 en_US


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