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Synthesis, biological evaluation and molecular docking of novel pyrazole derivatives as potent carbonic anhydrase and acetylcholinesterase inhibitors

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dc.contributor.author Turkan, Fiket
dc.contributor.author Çetin, Adnan
dc.contributor.author Taslimi, Parham
dc.contributor.author Karaman, Muhammet
dc.contributor.author Gülçin, İlhami
dc.date.accessioned 2019-04-25T09:15:36Z
dc.date.available 2019-04-25T09:15:36Z
dc.date.issued 2019-05
dc.identifier.issn 0045-2068
dc.identifier.uri https://www.sciencedirect.com/science/article/pii/S0045206818314202?via%3Dihub
dc.identifier.uri http://hdl.handle.net/11772/1080
dc.description.abstract A series of substituted pyrazole compounds (1–8 and 9a, b) were synthesized and their structure was characterized by IR, NMR, and Mass analysis. These obtained novel pyrazole derivatives (1–8 and 9a, b) were emerged as effective inhibitors of the cytosolic carbonic anhydrase I and II isoforms (hCA I and II) and acetylcholinesterase (AChE) enzymes with Ki values in the range of 1.03 ± 0.23–22.65 ± 5.36 µM for hCA I, 1.82 ± 0.30–27.94 ± 4.74 µM for hCA II, and 48.94 ± 9.63–116.05 ± 14.95 µM for AChE, respectively. Docking studies were performed for the most active compounds, 2 and 5, and binding mode between the compounds and the receptors were determined. en_US
dc.language.iso eng en_US
dc.publisher Elsevier en_US
dc.relation.isversionof 10.1016/j.bioorg.2019.02.013 en_US
dc.rights info:eu-repo/semantics/openAccess en_US
dc.subject Substituted pyrazole en_US
dc.subject Acetylcholinesterase en_US
dc.subject Carbonic anhydrase en_US
dc.subject Enzyme inhibition en_US
dc.title Synthesis, biological evaluation and molecular docking of novel pyrazole derivatives as potent carbonic anhydrase and acetylcholinesterase inhibitors 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 86 en_US
dc.identifier.startpage 420 en_US
dc.identifier.endpage 427 en_US


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