Multitarget drug discovery is an emerging approach to the design of new drugs to treat Alzheimer's disease. Using this strategy, we developed a series of dimeric ligands derived from the lead candidate bis(7)-tacrine (1), for which a multifunctional profile has been disclosed. These derivatives were evaluated at validated targets, namely cholinesterases and amyloid production and aggregation. Compound 3 resulted more effective than 1 in inhibiting BACE-1 activity and amyloid self-aggregation.
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Bolognesi et al. (2010) studied this question.
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