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dc.contributor.authorZondagh, Luke S.
dc.contributor.authorMalan, Sarel F.
dc.contributor.authorJoubert, Jacques
dc.date.accessioned2021-01-25T13:22:57Z
dc.date.available2021-01-25T13:22:57Z
dc.date.issued2020
dc.identifier.citationZondagh, L. S. et al. (2020). Design, synthesis and biological evaluation of edaravone derivatives bearing the N-benzyl pyridinium moiety as multifunctional anti-Alzheimer’s agents. Journal of Enzyme Inhibition and Medicinal Chemistry, 35(1), 1596-1605en_US
dc.identifier.issn1475-6374
dc.identifier.uri10.1080/14756366.2020.1801673
dc.identifier.urihttp://hdl.handle.net/10566/5758
dc.description.abstractA series of multi-target directed edaravone derivatives bearing N-benzyl pyridinium moieties were designed and synthesised. Edaravone is a potent antioxidant with significant neuroprotective effects and N-benzyl pyridinium has previously exhibited positive results as part of a dual-site binding, peripheral anionic site (PAS) and catalytic anionic site (CAS), acetylcholinesterase (AChE) inhibitor. The designed edaravone-N-benzyl pyridinium hybrid compounds were docked within the AChE active site. The results indicated interactions with conserved amino acids (Trp279 in PAS and Trp84 in CAS), suggesting good dual-site inhibitory activity. Significant in vitro AChE inhibitory activities were observed for selected compounds (IC50: 1.2–4.6 µM) with limited butyrylcholinesterase inhibitory activity (IC50’s >160 µM), indicating excellent selectivity towards AChE (SI: 46–>278). The compounds also showed considerable antioxidant ability, similar to edaravone.en_US
dc.language.isoenen_US
dc.publisherTaylor & Francisen_US
dc.subjectAlzheimer’s diseaseen_US
dc.subjectCholinesteraseen_US
dc.subjectEdaravoneen_US
dc.subjectN-benzyl pyridiniumen_US
dc.subjectOxidative stressen_US
dc.titleDesign, synthesis and biological evaluation of edaravone derivatives bearing the N-benzyl pyridinium moiety as multifunctional anti-Alzheimer’s agentsen_US
dc.typeArticleen_US


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