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

Authors :
Meleddu R
Fais A
Era B
Floris S
Distinto S
Lupia A
Cottiglia F
Onali A
Sanna E
Secci D
Atzeni G
Demuru L
Caboni P
Valenti D
Maccioni E
Source :
ACS medicinal chemistry letters [ACS Med Chem Lett] 2024 Sep 27; Vol. 15 (10), pp. 1685-1691. Date of Electronic Publication: 2024 Sep 27 (Print Publication: 2024).
Publication Year :
2024

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 <subscript>50</subscript> 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.<br />Competing Interests: The authors declare no competing financial interest.<br /> (© 2024 American Chemical Society.)

Details

Language :
English
ISSN :
1948-5875
Volume :
15
Issue :
10
Database :
MEDLINE
Journal :
ACS medicinal chemistry letters
Publication Type :
Academic Journal
Accession number :
39411531
Full Text :
https://doi.org/10.1021/acsmedchemlett.4c00246