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

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

  • ACS Med Chem Lett. 2024 Sep 27;15(10):1685-1691. doi: 10.1021/acsmedchemlett.4c00246.
Rita Meleddu 1,  Antonella Fais 1,  Benedetta Era 1,  Sonia Floris 1,  Simona Distinto 1,  Antonio Lupia 1 2,  Filippo Cottiglia 1,  Alessia Onali 1,  Erica Sanna 1,  Daniela Secci 1,  Giulia Atzeni 1,  Laura Demuru 1,  Pierluigi Caboni 1,  Donatella Valenti 1,  Elias Maccioni 1
Affiliations

Affiliations

  • 1 Department of Life and Environmental Sciences, University of Cagliari, University Campus, S.P. 8 km 0.700, 09042 Monserrato, Italy.
  • 2 Net4Science Srl, University "Magna Græcia", Campus Salvatore Venuta, Viale Europa, 88100, Catanzaro Italy.
PMID: 39411531 DOI: 10.1021/acsmedchemlett.4c00246
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.

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