@article {499,
	title = {Synthesis, Biological Evaluation and Molecular Modeling of Donepezil and N-[(5-(Benzyloxy)-1-methyl-1H-indol-2-yl)methyl]-N-methylprop-2-yn-1-amine Hybrids, as New Multipotent Cholinesterase/Monoamine Oxidase Inhibitors for the Treatment of Alzheimer{\textquoteright}s Di},
	journal = {Journal of medicinal chemistry},
	year = {2011},
	month = {2011/10/24/},
	abstract = {A new family of multi-target molecules able to interact with acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), as well as with monoamino oxidase (MAO) A and B has been synthesized. Novel compounds (3-9) have been designed using a conjunctive approach that combines the benzyl piperidine moiety of the AChE inhibitor donepezil (1), and the indolyl propargylamino moiety of the MAO inhibitor N-[(5-benzyloxy-1-methyl-1H-indol-2-yl)methyl]-N-methylprop-2-yn-1-amine (2), connected through an oligomethylene linker. The most promising hybrid (5) is a potent inhibitor of both MAO-A (IC50= 5.2 +/- 1.1 nM) and MAO-B (IC50= 43.1 +/- 7.9 nM), and a moderately potent inhibitor of AChE (IC50= 0.35 +/- 0.01 M) and BuChE (IC50= 0.46 +/- 0.06 M). Moreover, molecular modeling and kinetic studies support the dual binding site to AChE, which explains the inhibitory effect exerted on A aggregation. Overall, the results suggest that the new compounds are promising multi-target drug candidates with potential impact for Alzheimer{\textquoteright}s disease therapy.},
	author = {Bolea,I. and Juarez-Jimenez,J. and Rios,C. de los and Chioua,M. and Pouplana,R. and F. J. Luque and Unzeta,M. and Marco-Contelles,J. and Samadi,A.}
}
