Finally, the activity profile for compound 1h (AChE IC50 = 6.03 nM, H3R Ki = 558 nM), compound 1q (H3R Ki = 151 nM, AChE IC50 = 1950 nM, and MAO-B IC50 = 1688 nM), and compound 1b (H3R Ki = 32 nM, AChE IC50 = 1330 nM), summed to the complete absence of neurotoxicity up to 25 μM, and the ability of neuroprotection for some compounds, suggests that this series can represent a valuable model for the development of new candidates of MTDLs for the treatment of Alzheimer’s disease. Here, ACHE is linked to early-onset autosomal dominant Alzheimer disease.