| Literature DB >> 25793650 |
Christophe Rochais1, Cédric Lecoutey1, Florence Gaven2,3,4, Patrizia Giannoni2,3,4, Katia Hamidouche5, Damien Hedou1, Emmanuelle Dubost1, David Genest1, Samir Yahiaoui1, Thomas Freret5, Valentine Bouet5, François Dauphin5, Jana Sopkova de Oliveira Santos1, Céline Ballandonne1, Sophie Corvaisier1,5, Aurélie Malzert-Fréon1, Remi Legay1, Michel Boulouard5, Sylvie Claeysen2,3,4, Patrick Dallemagne1.
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.Entities:
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Year: 2015 PMID： 25793650 DOI： 10.1021/acs.jmedchem.5b00115
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446