%0 Journal Article
%A Ramos Alonso, Eva
%A Palomino-Antolín, Alejandra
%A Bartolini, Manuela
%A Iriepa, Isabel
%A Moraleda, Ignacio
%A Diez-Iriepa, Daniel
%A Samadi, Abdelouahid
%A Cortina, Carol V.
%A Chioua, Mourad
%A Egea, Javier
%A Romero Martínez, Manuel Alejandro
%A Marco-Contelles, José
%T QuinoxalineTacrine QT78, a Cholinesterase Inhibitor as a Potential Ligand for Alzheimer’s Disease Therapy
%D 2019
%@ 1420-3049
%U https://hdl.handle.net/20.500.14352/12527
%X We report the synthesis and relevant pharmacological properties of the quinoxalinetacrine (QT) hybrid QT78 in a project targeted to identify new non-hepatotoxic tacrine derivatives for Alzheimer’s disease therapy. We have found that QT78 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 (IC50 (hAChE) = 22.0 ± 1.3 μM; IC50 (hBuChE) = 6.79 ± 0.33 μM). Moreover, QT78 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.
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