Ricerc@Sapienza

In the last years the continuous efforts in the development of novel and effective inhibitors of human
monoamine oxidases (hMAOs) promoted the discovery of new agents able to effectively and selectively
bound one of the two isoforms (hMAO-A and hMAO-B). However, the parent chalcone scaffold still
covers an important role in hMAOs inhibition. In the present work, we focused our attention on the
researches performed in the last five years, involving chalcones or compounds that can be correlated to
them. We classified the chalcones into different groups depending on their structural characteristics or
common molecular properties. In this regard, we also considered chalcones based on heterocycles and
compounds endowed with scaffolds containing a masked chalcone motif. When structural attributes
could not be used, we took advantage of enzymatic activity to arrange compounds in a group. We followed
this approach for the multitarget agents. Finally, we also analysed the naturally occurring chalcones.
All the sections were discussed exhaustively and the structure-activity relationship (SAR) analyses
were sustained by means of detailed images describing the effects related to the substituents or structural
changes.