2026-06-29T01:17:55Zhttps://docta.ucm.es/rest/oai/request

oai:docta.ucm.es:20.500.14352/125272023-08-28T14:42:16Zcom_20.500.14352_14col_20.500.14352_15

QuinoxalineTacrine QT78, a Cholinesterase Inhibitor as a Potential Ligand for Alzheimer’s Disease Therapy Ramos Alonso, Eva Palomino-Antolín, Alejandra Bartolini, Manuela Iriepa, Isabel Moraleda, Ignacio Diez-Iriepa, Daniel Samadi, Abdelouahid Cortina, Carol V. Chioua, Mourad Egea, Javier Romero Martínez, Manuel Alejandro Marco-Contelles, José 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. 2023-06-17T12:34:24Z 2023-06-17T12:34:24Z 2023-06-17T12:34:24Z 2019-04-17 journal article https://hdl.handle.net/20.500.14352/12527 1420-3049 10.3390/molecules24081503 eng (SAF2006-08764-C02-01 and ISCIII [RED RENEVAS (RD06/0026/1002)) MIguel Servet CP14/00008;PI16/00735) https://creativecommons.org/licenses/by/3.0/es/ open access Atribución 3.0 España MDPI