RT Journal Article
T1 QuinoxalineTacrine QT78, a Cholinesterase Inhibitor as a Potential Ligand for Alzheimer’s Disease Therapy
A1 Ramos Alonso, Eva
A1 Palomino-Antolín, Alejandra
A1 Bartolini, Manuela
A1 Iriepa, Isabel
A1 Moraleda, Ignacio
A1 Diez-Iriepa, Daniel
A1 Samadi, Abdelouahid
A1 Cortina, Carol V.
A1 Chioua, Mourad
A1 Egea, Javier
A1 Romero Martínez, Manuel Alejandro
A1 Marco-Contelles, José
AB 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.
PB MDPI
SN 1420-3049
YR 2019
FD 2019-04-17
LK https://hdl.handle.net/20.500.14352/12527
UL https://hdl.handle.net/20.500.14352/12527
LA eng
NO Ministerio de Ciencia e Innovación (MICINN)
NO Instituto de Salud Carlos III/FEDER (European Regional Development Fund)
NO Fundación Mutua Madrileña
DS Docta Complutense
RD 28 abr 2025