Exploring\nthe 1‑(4-Nitrophenyl)-3-arylprop-2-en-1-one\nScaffold for the Selective Inhibition of Monoamine Oxidase B

A small library of 1-(4-nitrophenyl)-3-arylprop-2-en-1-one\nderivatives\nwas synthesized to identify new human monoamine oxidase B selective\ninhibitors. Their inhibitory activity toward MAO-A and MAO-B isoforms\nwas evaluated to determine their potency and selectivity. All newly\nsynthesized compounds were nanomolar inhibitors of the B isoform with\nIC<sub>50</sub> concentrations ranging from 120 to 2.2 nM. Conversely,\ntheir activity toward the A isozyme was only observed at micromolar\nconcentrations. Our results bear out the hypothesis that the 1,3-diarylpropenone\nscaffold could represent a valuable starting point for designing efficient\nand selective MAO-B inhibitors.