Abstract

Neurodegenerative disorders, such as Alzheimer’s and Parkinson’s, are very complex diseases, whose treatment and prevention are still very problematic to date. The search for new potential treatments is always a current topic. In this context, the discovery of molecules with a dual-targeting action against both MAO-B enzyme and A2A receptor has been largely pursued in recent years, considering their involvement in the etiological process of these diseases. In particular, caffeine, an alkaloid largely present in beverages and foods, has been shown to possess beneficial effects in the prevention/treatment of neurodegenerative disorders. Moreover, in vitro assays have confirmed its interaction with the MAO-B enzyme and A2A receptor, stimulating the synthesis of caffeine chemical derivatives that can strongly act against these two targets. In this chapter, several classes of caffeine derivatives have been discussed, with particular attention on their synthesis and (dual) biological activity of MAO-B enzyme and A2A receptor.