Novel Multitarget-Directed Ligands (MTDLs) with Acetylcholinesterase (AChE) Inhibitory and Serotonergic Subtype 4 Receptor (5-HT4R) Agonist Activities As Potential Agents against Alzheimer’s Disease: The Design of Donecopride

In this work, we describe the synthesis and in vitro evaluation of a novel series of multitarget-directed ligands (MTDL) displaying both nanomolar dual-binding site (DBS) acetylcholinesterase inhibitory effects and partial 5-HT4R agonist activity, among which donecopride was selected for further in...

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Veröffentlicht in:	Journal of medicinal chemistry 2015-04, Vol.58 (7), p.3172-3187
Hauptverfasser:	Rochais, Christophe, Lecoutey, Cédric, Gaven, Florence, Giannoni, Patrizia, Hamidouche, Katia, Hedou, Damien, Dubost, Emmanuelle, Genest, David, Yahiaoui, Samir, Freret, Thomas, Bouet, Valentine, Dauphin, François, Sopkova de Oliveira Santos, Jana, Ballandonne, Céline, Corvaisier, Sophie, Malzert-Fréon, Aurélie, Legay, Remi, Boulouard, Michel, Claeysen, Sylvie, Dallemagne, Patrick
Format:	Artikel
Sprache:	eng
Schlagworte:	Alzheimer Disease - drug therapy Aniline Compounds - administration & dosage Aniline Compounds - chemistry Aniline Compounds - pharmacology Animals Chemical Sciences Cholinesterase Inhibitors - chemistry Cholinesterase Inhibitors - pharmacology Computer Simulation Crystallography, X-Ray Drug Design Drug Evaluation, Preclinical - methods Guinea Pigs Humans Ligands Male Medicinal Chemistry Memory, Short-Term - drug effects Mice, Inbred C57BL Mice, Inbred Strains Molecular Targeted Therapy Piperidines - administration & dosage Piperidines - chemistry Piperidines - pharmacology Receptors, Serotonin, 5-HT4 - metabolism Serotonin 5-HT4 Receptor Agonists - chemistry Serotonin 5-HT4 Receptor Agonists - pharmacology Structure-Activity Relationship Toxicity Tests, Acute
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