期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 58, 期 7, 页码 3172-3187出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.5b00115
关键词
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资金
- Conseil Regional de Basse Normandie, France (Dispositif de Soutien aux Projets de Recherche Emergents)
- French Agence Nationale de la Recherche [MALAD ANR-12-JS007-0012-01, ADAMGUARD ANR-12-BSV4-008-01]
- Ligue Europeenne Contre la Maladie d'Alzheimer Grant [12721]
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 sAPPa release, accounting for a potential symptomatic and disease-modifying therapeutic benefit in the treatment of Alzheimers disease.
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