Tacripyrines, the First Tacrine−Dihydropyridine Hybrids, as Multitarget-Directed Ligands for the Treatment of Alzheimer’s Disease

Tacripyrines (1−14) have been designed by combining an AChE inhibitor (tacrine) with a calcium antagonist such as nimodipine and are targeted to develop a multitarget therapeutic strategy to confront AD. Tacripyrines are selective and potent AChE inhibitors in the nanomolar range. The mixed type inh...

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Veröffentlicht in:	Journal of medicinal chemistry 2009-05, Vol.52 (9), p.2724-2732
Hauptverfasser:	Marco-Contelles, José, León, Rafael, de los Ríos, Cristóbal, Samadi, Abdelouahid, Bartolini, Manuela, Andrisano, Vincenza, Huertas, Oscar, Barril, Xavier, Luque, F. Javier, Rodríguez-Franco, María I, López, Beatriz, López, Manuela G, García, Antonio G, do Carmo Carreiras, María, Villarroya, Mercedes
Format:	Artikel
Sprache:	eng
Schlagworte:	Acetylcholinesterase - metabolism Alzheimer Disease - drug therapy Alzheimer Disease - enzymology Alzheimer Disease - metabolism Alzheimer Disease - pathology Amyloid beta-Peptides - metabolism Biological and medical sciences Blood-Brain Barrier - drug effects Blood-Brain Barrier - metabolism Butyrylcholinesterase - metabolism Calcium - metabolism Calcium Channel Blockers - chemistry Calcium Channel Blockers - metabolism Calcium Channel Blockers - pharmacology Calcium Channel Blockers - therapeutic use Catalytic Domain Cell Death - drug effects Cell Line, Tumor Cholinesterase Inhibitors - chemistry Cholinesterase Inhibitors - metabolism Cholinesterase Inhibitors - pharmacology Cholinesterase Inhibitors - therapeutic use Cytosol - drug effects Cytosol - metabolism Dihydropyridines - chemistry Dihydropyridines - metabolism Dihydropyridines - pharmacology Dihydropyridines - therapeutic use Humans Hydrogen Peroxide - metabolism Kinetics Ligands Medical sciences Models, Molecular Neuropharmacology Neuroprotective agent Peptide Fragments - metabolism Permeability - drug effects Pharmacology. Drug treatments Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease) Psychology. Psychoanalysis. Psychiatry Psychopharmacology Tacrine - analogs & derivatives
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