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DOI 10.1021/acs.jmedchem.5b00115

Медицинская библиотека · Journal of medicinal chemistry · 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.

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

СтатьяПоддержка исследования: вне правительства СШАПеревод пока не подготовлен

Аннотация

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.

Для цитирования: 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. 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. 2015. DOI: 10.1021/acs.jmedchem.5b00115.

Предметные рубрики MeSH

Alzheimer DiseaseAniline CompoundsAnimalsCholinesterase InhibitorsComputer SimulationCrystallography, X-RayDrug DesignDrug Evaluation, PreclinicalGuinea PigsHumansLigandsMaleMemory, Short-TermMice, Inbred C57BLMice, Inbred StrainsMolecular Targeted TherapyPiperidinesReceptors, Serotonin, 5-HT4Serotonin 5-HT4 Receptor AgonistsStructure-Activity RelationshipToxicity Tests, Acute
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