Melatonin is a key regulatory hormone produced mainly in the pineal gland. In the recent years, melatonin contribution to neurodegenerative disorders has dramatically increased when inspecting its favorable pharmacological profile. Its levels were found to be decreased during aging. Data from clinical studies point out to its positive outcome not only in improving the quality of sleep but it also exerts anti-inflammatory and antioxidant profile. Moreover, it was found as an effective neuroprotective agent. Current study summarizes the experimental data from basic research of medicinal chemistry field devoted to melatonin. Particular emphasis is directed toward melatonin derivatives with multipotent profile affecting concomitantly several pathological hallmarks of the neurodegenerative disorders. Key words: acetylcholinesterase • Alzheimer's disease • antioxidant • butyrylcholinesterase • melatonin • neurodegenerative disorders.