Indolyl imine compounds as multi-target agents; synthesis, antidiabetic, anticholinesterase, antioxidant activities and molecular modeling

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dc.contributor.authorCeyhan, Sadık M.
dc.contributor.authorZengin, İrem Nur
dc.contributor.authorBingül, Murat
dc.contributor.authorŞahin, Hasan
dc.contributor.authorBoǧa, Mehmet
dc.contributor.authorSağlam, Mehmet F.
dc.contributor.authorKandemir, Hakan
dc.date.accessioned2024-04-24T17:56:09Z
dc.date.available2024-04-24T17:56:09Z
dc.date.issued2024
dc.departmentDicle Üniversitesi, Eczacılık Fakültesi, Temel Eczacılık Bilimleri Bölümüen_US
dc.description.abstractA new range of indolyl imine system 3d-l has been successfully prepared from 4,6-dimethoxy-2,3-diphenyl-indole-7-carbaldehyde 2a and 4,6-dimethoxy-3-aryl-indole-7-carbaldehyde 2b-c via Schiff base reaction. The structure of targeted compounds was confirmed by 1H and 13C NMR, FT-IR, mass spectrometry and single crystal X-ray diffraction techniques. The indolyl imine derivatives were also subjected to in vitro antidiabetic activities employing ?-glucosidase and ?-amylase enzymes. In terms of antidiabetic investigation, the ?-glucosidase enzyme was found to be potential target due to the comparable inhibition concentrations with the standard acarbose and the compound 3e exhibited better potency than the standard. The anticholinesterase potency of the compounds was investigated towards the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. The compounds displayed moderate efficiency against the BChE enzyme with the best inhibition concentration of 30.48 ?M by the compound 3h. The antioxidant properties of final compounds were determined by DPPH radical scavenging, ABTS Cation Radical Decolarization and CUPRAC Cupric Reducing Antioxidant Capacity assay methods. The ABTS cation scavenging assay provided the best responses for the compounds and the candidates 3k and 3l were determined as promising targets for the antioxidant activity. Plausible binding mode and interaction of ligands with the selected enzyme have been studied by molecular docking, supporting the experimental results. In silico ADME showed high drug likeness of the synthesized compounds. © 2024 Elsevier B.V.en_US
dc.description.sponsorshipGebze Teknik Üniversitesi: 2021-A101-04en_US
dc.description.sponsorshipThis work has been supported by Research Found of the Gebze Technical University (Project Number: 2021-A101-04).en_US
dc.identifier.citationCeyhan, S. M., Zengin, İ. N., Bingül, M., Şahin, H., Boğa, M., Sağlam, M. F. ve diğerleri. (2024). Indolyl imine compounds as multi-target agents; synthesis, antidiabetic, anticholinesterase, antioxidant activities and molecular modeling. Journal of Molecular Structure, 1309, 1-14.
dc.identifier.doi10.1016/j.molstruc.2024.138159
dc.identifier.issn0022-2860
dc.identifier.scopus2-s2.0-85189090245
dc.identifier.scopusqualityQ1
dc.identifier.urihttps://doi.org/10.1016/j.molstruc.2024.138159
dc.identifier.urihttps://hdl.handle.net/11468/23335
dc.identifier.volume1309en_US
dc.indekslendigikaynakScopus
dc.institutionauthorBingül, Murat
dc.institutionauthorŞahin, Hasan
dc.institutionauthorBoǧa, Mehmet
dc.language.isoenen_US
dc.publisherElsevier B.V.en_US
dc.relation.ispartofJournal of Molecular Structure
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectAnticholinesteraseen_US
dc.subjectAntioxidanten_US
dc.subjectIndoleen_US
dc.subjectMolecular modelingen_US
dc.subjectα-Amylaseen_US
dc.subjectα-Glucosidaseen_US
dc.titleIndolyl imine compounds as multi-target agents; synthesis, antidiabetic, anticholinesterase, antioxidant activities and molecular modelingen_US
dc.titleIndolyl imine compounds as multi-target agents; synthesis, antidiabetic, anticholinesterase, antioxidant activities and molecular modeling
dc.typeArticleen_US

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