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J Enzyme Inhib Med Chem. 2019 Dec;34(1):479-489. doi: 10.1080/14756366.2018.1545766.

Donepezil + chromone + melatonin hybrids as promising agents for Alzheimer's disease therapy.

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a Neurosciences intégratives et cliniques, Pôle Chimie Organique et Thérapeutique , University Bourgogne Franche-Comté , Besançon , France.
b Faculty of Science, Department of Chemistry , University of Hradec Kralove , Hradec Kralove , Czech Republic.
c PEPITE EA4267, Laboratoire de Toxicologie Cellulaire , University Bourgogne Franche-Comté , Besançon , France.
d Department of Organic Chemistry and Inorganic Chemistry , Alcalà University , Madrid , Spain.
e Institute of Chemical Research Andrés M. del Río , Alcalà University , Madrid , Spain.
f Instituto de Investigación en Neuroquímica , Universidad Complutense de Madrid , Madrid , Spain.
g Department of Biochemistry and Molecular Biology, School of Pharmacy , Plaza de Ramòn y Cajal , Madrid , Spain.
h Laboratory of Medicinal Chemistry (IQOG, CSIC) , Madrid , Spain.


We describe herein the design, multicomponent synthesis and biological studies of new donepezil + chromone + melatonin hybrids as potential agents for Alzheimer's disease (AD) therapy. We have identified compound 14n as promising multitarget small molecule showing strong BuChE inhibition (IC50 = 11.90 ± 0.05 nM), moderate hAChE (IC50 = 1.73 ± 0.34 μM), hMAO A (IC50 = 2.78 ± 0.12 μM), and MAO B (IC50 = 21.29 ± 3.85 μM) inhibition, while keeping a strong antioxidant power (3.04 TE, ORAC test). Consequently, the results reported here support the development of new multitarget Donepezil + Chromone + Melatonin hybrids, such as compound 14n, as a potential drug for AD patients cure.


Antioxidant; MAO-A; MAO-B; ORAC; Ugi-4MCR; cholinesterases; donepezil

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