In the context of the search for multitarget drugs with improved efficacy against neurodegenerative disorders, carbohydrate derivatives have emerged as promising candidates for Alzheimer's therapy. Herein we describe the synthesis and biological evaluation of several classes of sugar-based compounds, where most of them contain heterocyclic aromatic moieties that bear known biological properties and high affinity for the cholinesterase active site. This general idea led to the synthesis of compounds with high inhibitory potency against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), enzymatic selectivity and combined properties such as antioxidant and neuroprotection, in addition to the absence of toxicity.