| Title : QuinoxalineTacrine QT78, a Cholinesterase Inhibitor as a Potential Ligand for Alzheimer's Disease Therapy - Ramos_2019_Molecules_24_ |
| Author(s) : Ramos E , Palomino-Antolin A , Bartolini M , Iriepa I , Moraleda I , Diez-Iriepa D , Samadi A , Cortina CV , Chioua M , Egea J , Romero A , Marco-Contelles J |
| Ref : Molecules , 24 : , 2019 |
|
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 muM to 1 mM), less potent than tacrine as a ChE inhibitor, but shows selective BuChE inhibition (IC50 (hAChE) = 22.0 +/- 1.3 muM; IC50 (hBuChE) = 6.79 +/- 0.33 muM). 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. |
| PubMedSearch : Ramos_2019_Molecules_24_ |
| PubMedID: 30999586 |
Ramos E, Palomino-Antolin A, Bartolini M, Iriepa I, Moraleda I, Diez-Iriepa D, Samadi A, Cortina CV, Chioua M, Egea J, Romero A, Marco-Contelles J (2019)
QuinoxalineTacrine QT78, a Cholinesterase Inhibitor as a Potential Ligand for Alzheimer's Disease Therapy
Molecules
24 :
Ramos E, Palomino-Antolin A, Bartolini M, Iriepa I, Moraleda I, Diez-Iriepa D, Samadi A, Cortina CV, Chioua M, Egea J, Romero A, Marco-Contelles J (2019)
Molecules
24 :