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Title

QuinoxalineTacrine QT78, a Cholinesterase Inhibitor as a Potential Ligand for Alzheimer’s Disease Therapy

AuthorsRamos, Eva; Palomino-Antolín, Alejandra; Bartolini, Manuela; Iriepa, Isabel; Moraleda, Ignacio; Diez-Iriepa, Daniel; Samadi, Abdelouahid ; Cortina, Carol V.; Chioua, Mourad ; Egea, Javier; Romero, Alejandro ; Marco-Contelles, José
KeywordsAlzheimer’s disease
Cholinesterase inhibitor
Hepatotoxicity
Molecular modeling
Neuroprotection
Quinoxalines
Quinoxalinetacrines
Tacrine
Issue Date17-Apr-2019
PublisherMultidisciplinary Digital Publishing Institute
CitationMolecules 24(8): 1503 (2019)
AbstractWe report the synthesis and relevant pharmacological properties of the quinoxalinetacrine (QT) hybrid <b>QT78</b> in a project targeted to identify new non-hepatotoxic tacrine derivatives for Alzheimer’s disease therapy. We have found that <b>QT78</b> is less toxic than tacrine at high concentrations (from 100 μM to 1 mM), less potent than tacrine as a ChE inhibitor, but shows selective BuChE inhibition (IC<sub>50</sub> (hAChE) = 22.0 ± 1.3 μM; IC<sub>50</sub> (hBuChE) = 6.79 ± 0.33 μM). Moreover, <b>QT78</b> showed effective and strong neuroprotection against diverse toxic stimuli, such as rotenone plus oligomycin-A or okadaic acid, of biological significance for Alzheimer’s disease.
Publisher version (URL)http://dx.doi.org/10.3390/molecules24081503
URIhttp://hdl.handle.net/10261/180729
DOI10.3390/molecules24081503
ISSN1420-3049
Appears in Collections:(IQOG) Artículos
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