Coumarin or benzoxazinone based novel carbonic anhydrase inhibitors: synthesis, molecular docking and anticonvulsant studies

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dc.authoridUSLU, HARUN/0000-0001-8827-8557
dc.authoridSARI, SUAT/0000-0002-8248-4218
dc.authoridGençer, Nahit/0000-0001-7092-8857
dc.authoridGençer, Nahit/0000-0001-7092-8857
dc.authoridSARI, SUAT/0000-0002-8248-4218
dc.authoridalagoz, mehmet abdullah/0000-0001-5190-7196
dc.authoridKarataş, Mert Olgun/0000-0001-8500-2088
dc.authorwosidUSLU, HARUN/P-3681-2019
dc.authorwosidSARI, SUAT/JCD-8070-2023
dc.authorwosidGençer, Nahit/HHD-1544-2022
dc.authorwosidGençer, Nahit/AAG-4507-2019
dc.authorwosidSARI, SUAT/A-5249-2017
dc.authorwosidalagoz, mehmet abdullah/W-7847-2018
dc.authorwosidKarataş, Mert Olgun/ABG-7848-2020
dc.contributor.authorKaratas, Mert Olgun
dc.contributor.authorUslu, Harun
dc.contributor.authorSari, Suat
dc.contributor.authorAlagoz, Mehmet Abdullah
dc.contributor.authorKarakurt, Arzu
dc.contributor.authorAlici, Bulent
dc.contributor.authorBilen, Cigdem
dc.date.accessioned2024-08-04T20:41:07Z
dc.date.available2024-08-04T20:41:07Z
dc.date.issued2016
dc.departmentİnönü Üniversitesien_US
dc.description.abstractAmong many others, coumarin derivatives are known to show human carbonic anhydrase (hCA) inhibitory activity. Since hCA inhibition is one of the underlying mechanisms that account for the activities of some antiepileptic drugs (AEDs), hCA inhibitors are expected to have anti-seizure properties. There are also several studies reporting compounds with an imidazole and/or benzimidazole moiety which exert these pharmacological properties. In this study, we prepared fifteen novel coumarin-bearing imidazolium and benzimidazolium chloride, nine novel benzoxazinone-bearing imidazolium and benzimidazolium chloride derivatives and evaluated their hCA inhibitory activities and along with fourteen previously synthesized derivatives we scanned their anticonvulsant effects. As all compounds inhibited purified hCA isoforms I and II, some of them also proved protective against Maximal electroshock seizure (MES) and ScMet induced seizures in mice. Molecular docking studies with selected coumarin derivatives have revealed that these compounds bind to the active pocket of the enzyme in a similar fashion to that previously described for coumarin derivatives.en_US
dc.identifier.doi10.3109/14756366.2015.1063624
dc.identifier.endpage772en_US
dc.identifier.issn1475-6366
dc.identifier.issn1475-6374
dc.identifier.issue5en_US
dc.identifier.pmid26207513en_US
dc.identifier.scopus2-s2.0-84939146964en_US
dc.identifier.scopusqualityQ1en_US
dc.identifier.startpage760en_US
dc.identifier.urihttps://doi.org/10.3109/14756366.2015.1063624
dc.identifier.urihttps://hdl.handle.net/11616/96908
dc.identifier.volume31en_US
dc.identifier.wosWOS:000379783700010en_US
dc.identifier.wosqualityQ1en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.language.isoenen_US
dc.publisherTaylor & Francis Ltden_US
dc.relation.ispartofJournal of Enzyme Inhibition and Medicinal Chemistryen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/openAccessen_US
dc.subjectAnticonvulsanten_US
dc.subjectbenzoxazinoneen_US
dc.subjectcarbonic anhydraseen_US
dc.subjectcoumarinen_US
dc.subjectepilepsyen_US
dc.subjectinhibitionen_US
dc.titleCoumarin or benzoxazinone based novel carbonic anhydrase inhibitors: synthesis, molecular docking and anticonvulsant studiesen_US
dc.typeArticleen_US

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