| Title : 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 - Rochais_2015_J.Med.Chem_58_3172 |
| Author(s) : Rochais C , Lecoutey C , Gaven F , Giannoni P , Hamidouche K , Hedou D , Dubost E , Genest D , Yahiaoui S , Freret T , Bouet V , Dauphin F , Sopkova de Oliveira Santos J , Ballandonne C , Corvaisier S , Malzert-Freon A , Legay R , Boulouard M , Claeysen S , Dallemagne P |
| Ref : Journal of Medicinal Chemistry , 58 :3172 , 2015 |
|
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 sAPPalpha release, accounting for a potential symptomatic and disease-modifying therapeutic benefit in the treatment of Alzheimer's disease. |
| PubMedSearch : Rochais_2015_J.Med.Chem_58_3172 |
| PubMedID: 25793650 |
| Inhibitor | Donecopride |
Rochais C, Lecoutey C, Gaven F, Giannoni P, Hamidouche K, Hedou D, Dubost E, Genest D, Yahiaoui S, Freret T, Bouet V, Dauphin F, Sopkova de Oliveira Santos J, Ballandonne C, Corvaisier S, Malzert-Freon A, Legay R, Boulouard M, Claeysen S, Dallemagne P (2015)
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
Journal of Medicinal Chemistry
58 :3172
Rochais C, Lecoutey C, Gaven F, Giannoni P, Hamidouche K, Hedou D, Dubost E, Genest D, Yahiaoui S, Freret T, Bouet V, Dauphin F, Sopkova de Oliveira Santos J, Ballandonne C, Corvaisier S, Malzert-Freon A, Legay R, Boulouard M, Claeysen S, Dallemagne P (2015)
Journal of Medicinal Chemistry
58 :3172