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. 2015 Apr 9;58(7):3172-87.
doi: 10.1021/acs.jmedchem.5b00115. Epub 2015 Mar 31.

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

Christophe Rochais  1 , Cédric Lecoutey  1 , Florence Gaven  2   3   4 , Patrizia Giannoni  2   3   4 , Katia Hamidouche  5 , Damien Hedou  1 , Emmanuelle Dubost  1 , David Genest  1 , Samir Yahiaoui  1 , Thomas Freret  5 , Valentine Bouet  5 , François Dauphin  5 , Jana Sopkova de Oliveira Santos  1 , Céline Ballandonne  1 , Sophie Corvaisier  1   5 , Aurélie Malzert-Fréon  1 , Remi Legay  1 , Michel Boulouard  5 , Sylvie Claeysen  2   3   4 , Patrick Dallemagne  1
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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

Christophe Rochais et al. J Med Chem. .
Free article

Abstract

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 vivo evaluations in mice. The latter displayed procognitive and antiamnesic effects and enhanced sAPPα release, accounting for a potential symptomatic and disease-modifying therapeutic benefit in the treatment of Alzheimer's disease.

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