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.
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