Focusing on AD, its structure has been combined by means of selected linkers with diverse heterocycles, often leading to promising compounds capable of engaging both the most predictable targets, namely AChE, BChE, MAO-B, GSK-3β and metals, and some unconventional and emerging ones, such as CB receptors and CA and FAAH enzymes, always proving to possess promising activity. Here, GSK3B is linked to Alzheimer disease.