Design, Synthesis, and Biological Evaluation of Some Benzothiazolone Derivatives as Cholinesterase Inhibitors

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dc.authoridSARI, SUAT/0000-0002-8248-4218
dc.authoridAKKAYA, Didem/0000-0002-0711-951X
dc.authoridOnkol, Tijen/0000-0003-3973-5728
dc.authoridOzdemir, Zenyep/0000-0003-4559-2305
dc.authoridSARI, SUAT/0000-0002-8248-4218
dc.authoridalagoz, mehmet abdullah/0000-0001-5190-7196
dc.authoridARSLAN, Gulnur/0000-0001-9054-7437
dc.authorwosidSARI, SUAT/A-5249-2017
dc.authorwosidAKKAYA, Didem/AAJ-7644-2021
dc.authorwosidOnkol, Tijen/AAA-2377-2021
dc.authorwosidOzdemir, Zenyep/AAJ-6384-2020
dc.authorwosidSARI, SUAT/JCD-8070-2023
dc.authorwosidalagoz, mehmet abdullah/W-7847-2018
dc.contributor.authorAlagoz, Mehmet Abdullah
dc.contributor.authorAkkaya, Didem
dc.contributor.authorArslan, Gulnur
dc.contributor.authorUludag, Berk
dc.contributor.authorOzdemir, Zeynep
dc.contributor.authorBarut, Burak
dc.contributor.authorOnkol, Tijen
dc.date.accessioned2024-08-04T20:53:15Z
dc.date.available2024-08-04T20:53:15Z
dc.date.issued2022
dc.departmentİnönü Üniversitesien_US
dc.description.abstractIn this study, nine new benzothiazolone derivatives (6 a-i) were designed and synthesized to identify potent cholinesterase inhibitors. The compounds were tested in vitro against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) and found to be selective to BChE. Compound 6 f proved the most potent derivative (IC50=12.25 +/- 0.23 mu M) against BChE and was identified as a mixed-type inhibitor with a K-i value of 4.45 +/- 0.35 mu M according to the kinetic studies. Molecular modelling suggested that the derivatives were druglike and non-PAINS. Compound 6 f showed good fit in BChE active site interacting with the key sites important for enzyme activity according to the molecular docking study.en_US
dc.identifier.doi10.1002/slct.202203250
dc.identifier.issn2365-6549
dc.identifier.issue46en_US
dc.identifier.scopus2-s2.0-85144216833en_US
dc.identifier.scopusqualityQ2en_US
dc.identifier.urihttps://doi.org/10.1002/slct.202203250
dc.identifier.urihttps://hdl.handle.net/11616/101067
dc.identifier.volume7en_US
dc.identifier.wosWOS:000894288900001en_US
dc.identifier.wosqualityQ3en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.language.isoenen_US
dc.publisherWiley-V C H Verlag Gmbhen_US
dc.relation.ispartofChemistryselecten_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectbenzothiazoloneen_US
dc.subjectcholinesterase inhibitionen_US
dc.subjectmolecular dockingen_US
dc.titleDesign, Synthesis, and Biological Evaluation of Some Benzothiazolone Derivatives as Cholinesterase Inhibitorsen_US
dc.typeArticleen_US

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