Journal
MOLECULES
Volume 24, Issue 8, Pages -Publisher
MDPI
DOI: 10.3390/molecules24081503
Keywords
Alzheimer's disease; cholinesterase inhibitor; hepatotoxicity; molecular modeling; neuroprotection; quinoxalines; quinoxalinetacrines; tacrine
Funding
- MICINN [SAF2006-08764-C02-01]
- ISCIII [RED RENEVAS] [RD06/0026/1002]
- Fondo de Investigaciones Sanitarias (FIS)(ISCIII/FEDER)(Programa MIguel Servet) [CP14/00008, PI16/00735]
- Fundacion Mutua Madrilena
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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 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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