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

Rita Meleddu

Primo

;Antonella Fais

;Benedetta Era;Sonia Floris;Simona Distinto;Antonio Lupia;Filippo Cottiglia;Alessia Onali;Erica Sanna;Daniela Secci;Giulia Atzeni;Laura Demuru;Pierluigi Caboni;Donatella Valenti;Elias Maccioni

2024-01-01

---

Abstract

A small library of 1-(4-nitrophenyl)-3-arylprop-2-en-1-one derivatives was synthesized to identify new human monoamine oxidase B selective inhibitors. Their inhibitory activity toward MAO-A and MAO-B isoforms was evaluated to determine their potency and selectivity. All newly synthesized compounds were nanomolar inhibitors of the B isoform with IC50 concentrations ranging from 120 to 2.2 nM. Conversely, their activity toward the A isozyme was only observed at micromolar concentrations. Our results bear out the hypothesis that the 1,3-diarylpropenone scaffold could represent a valuable starting point for designing efficient and selective MAO-B inhibitors.