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

descriptionPublicationkeyboard_double_arrow_right Article , Other literature type 17 Apr 2019 Spain, Italy English Publisher:MDPI AGJournal:Molecules, volume 24, page 1,503 (eissn: 1420-3049,

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Authors: Eva Ramos; Alejandra Palomino-Antolín; Manuela Bartolini; Isabel Iriepa; Ignacio Moraleda; Daniel Diez-Iriepa; Abdelouahid Samadi; +5 Authors

doi: 10.3390/molecules24081503

pmid: 30999586

pmc: PMC6514705

handle: 20.500.12530/73219 , 10486/691168 , 20.500.14352/12527 , 10261/180729 , 11585/726220

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

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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.

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Spain, Italy

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Keywords

Farmacología veterinaria, hepatotoxicity, Alzheimer’s disease; Cholinesterase inhibitor; Hepatotoxicity; Molecular modeling; Neuroprotection; Quinoxalines; Quinoxalinetacrines; Tacrine; Alzheimer Disease; Hep G2 Cells; Humans; Cholinesterase Inhibitors; Tacrine, 3109.08 Farmacología, Neurociencias, Organic chemistry, Molecular modeling, tacrine, Quinoxalinetacrines, Article, Neurociencias (Medicina), QD241-441, Alzheimer Disease, Quinoxalines, cholinesterase inhibitor, Humans, molecular modeling, Hepatotoxicity, Cholinesterase inhibitors, Hep G2 Cells, Cholinesterase inhibitor, Farmacia, Neuroprotection, 2490 Neurociencias, Tacrine, neuroprotection, quinoxalines, quinoxalinetacrines, Cholinesterase Inhibitors, Alzheimer’s disease

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