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

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 IC<sub>50</sub> 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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Publication Details

Journal
ACS Medicinal Chemistry Letters
Published
2024-09-27
DOI
https://doi.org/10.1021/acsmedchemlett.4c00246
Citations
1
Primary Topic
Neuroscience and Neuropharmacology Research
Type
article
Field-Weighted Citation Impact
0.27
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article

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

Simona Distinto, Sonia Floris, Donatella Valenti, Benedetta Era et al.
1 citations
ACS Medicinal Chemistry Letters
Neuroscience and Neuropharmacology Research
0.27
article

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

Simona Distinto, Sonia Floris, Donatella Valenti, Benedetta Era, Elias Maccioni, Antonio Lupia, Filippo Cottiglia, Antonella Fais, Alessia Onali, Daniela Secci, Erica Sanna, Rita Meleddu, Giulia Atzeni, Pierluigi Caboni, Laura Demuru
article en
1 citations

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 IC<sub>50</sub> 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.

ACS Medicinal Chemistry LettersVol. 15(10)
University of Cagliari (IT), Magna Graecia University (IT)
Openalex Percentile: Top 44%
Neuroscience and Neuropharmacology Research
0.27
DOIOpen Access PDFOpenAlex
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Exploring the 1-(4-Nitrophenyl)-3-arylprop-2-en-1-one Scaffold for the Selective Inhibition of Monoamine Oxidase B — Simona Distinto, Sonia Floris, et al. · ACS Medicinal Chemistry Letters (2024) | TGRS Research Map | TGRS