Quinoxalinetacrine QT78, a cholinesterase inhibitor as a potential ligand for Alzheimer’s disease therapy
Entity
UAM. Departamento de Farmacología; Instituto de Investigación del Hospital de La Princesa (IP); UAM. Instituto Teófilo Hernando de I+D del Medicamento (ITH)Publisher
MDPIDate
2019-04-17Citation
10.3390/molecules24081503
Molecules 24 (2019): 1503
ISSN
1420-3049 (print); 1420-3049 (online)DOI
10.3390/molecules24081503Funded by
J.M.-C is indebted to MICINN (SAF2006-08764-C02-01 and ISCIII [RED RENEVAS (RD06/0026/1002)] for financial support. Also this work was supported by grants from Fondo de Investigaciones Sanitarias (FIS)(ISCIII/FEDER)(Programa MIguel Servet CP14/00008;PI16/00735) and Fundación Mutua Madrileña to J.E.Editor's Version
https://doi.org/10.3390/molecules24081503Subjects
Alzheimer’s disease; Cholinesterase inhibitor; Hepatotoxicity; Molecular modeling; Neuroprotection; Quinoxalines; Quinoxalinetacrines; Tacrine; FarmaciaRights
© 2019 by the authors. Licensee MDPI, Basel, SwitzerlandAbstract
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 _M to 1 mM), less potent than tacrine as a ChE inhibitor, but shows selective BuChE
inhibition (IC50 (hAChE) = 22.0 _ 1.3 _M; IC50 (hBuChE) = 6.79 _ 0.33 _M). Moreover, QT78 showed
e_ective and strong neuroprotection against diverse toxic stimuli, such as rotenone plus oligomycin-A
Files in this item
Google Scholar:Ramos, Eva
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Palomino-Antolín, Alejandra
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Bartolini, Manuela
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Iriepa, Isabel
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Moraleda, Ignacio
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Diez-Iriepa, Daniel
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Samadi, Abdelouahid
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Cortina, Carol V.
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Chioua, Mourad
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Egea, Javier
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Romero, Alejandro
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Marco-Contelles, José
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