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

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Ramos Alonso, Eva and Palomino-Antolín, Alejandra and Bartolini, Manuela and Iriepa, Isabel and Moraleda, Ignacio and Diez-Iriepa, Daniel and Samadi, Abdelouahid and Cortina, Carol V. and Chioua, Mourad and Egea, Javier and Romero Martínez, Manuel Alejandro and Marco-Contelles, José (2019) QuinoxalineTacrine QT78, a Cholinesterase Inhibitor as a Potential Ligand for Alzheimer’s Disease Therapy. Molecules, 24 (8). p. 1503. ISSN 1420-3049

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Official URL: https://doi.org/10.3390/molecules24081503




Abstract

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.


Item Type:Article
Uncontrolled Keywords:Alzheimer’s disease; cholinesterase inhibitor; hepatotoxicity; molecular modeling; neuroprotection; quinoxalines; quinoxalinetacrines; tacrine
Subjects:Medical sciences > Medicine > Neurosciences
Medical sciences > Veterinary > Veterinary pharmacology
ID Code:65102
Deposited On:26 Apr 2021 15:49
Last Modified:27 Apr 2021 06:57

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