Ricerc@Sapienza

A new series of 4-(3-nitrophenyl)thiazol-2-ylhydrazone derivatives were designed, synthesised, and evaluated to assess their inhibitory effect on the human monoamine oxidase (hMAO) A and B isoforms. Different (un)substituted (hetero)aromatic substituents were linked to N1 of the hydrazone in order to establish robust structure–activity relationships.

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