Tacrine was the first drug approved by FDA for the treatment of Alzheimer’s disease. However, its use was
restricted in function of side effects observed in some patients. Investigations on the structural basis by which tacrine inhibits
cholinesterases activity brought new perspectives for the design of more potent analogs with fewer side effects. This
review discusses the recent advances on the development of tacrine-structure-based compounds capable to target multiple
molecules involved in Alzheimer’s disease. Detailed information on strategies of molecular modifications commonly used
in medicinal chemistry, such as bioisosterism, hybridization, dimerization and simplification is presented as well.
Keywords: Alzheimer's disease, tacrine, bioisosterism, dimerization, hybridization, molecular simplification, multi target directed ligands
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