The primary goal of the project is to develop molecules with the potential to alleviate the symptoms and slow down the progression of neurodegenerative diseases (ND) that primarily affect the neurons in the human brain that causes problems with mental functioning. The project aims to rationally design dual site binding cholinesterase (ChE) inhibitors (acting on improving the acetyl choline level in the brain and on Aβ aggregation) and use them as starting points for multitarget-directed ligand (MTDL) design by adding an additional pharmacophore in a single molecule entity able to act on other hallmarks of Alzheimer’s type of dementia. Compounds will be biologically evaluated (BACE1 and Aβ-aggregation inhibition, pro-oxidant/antioxidant capacity, cytotoxicity, etc.) to determine their ability as possible drugs for treatment of ND. The development of these designed compounds will have two major objectives: development of CNS active and development of peripherally active compounds, depending on their ability to cross the blood-brain-barrier.