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