Reversible Small Molecule Inhibitors of MAO A and MAO B with Anilide Motifs.

ABSTRACT:

Background

Ligands consisting of two aryl moieties connected via a short spacer were shown to be potent inhibitors of monoamine oxidases (MAO) A and B, which are known as suitable targets in treatment of neurological diseases. Based on this general blueprint, we synthesized a series of 66 small aromatic amide derivatives as novel MAO A/B inhibitors.

Methods

The compounds were synthesized, purified and structurally confirmed by spectroscopic methods. Fluorimetric enzymological assays were performed to determine MAO A/B inhibition properties. Mode and reversibility of inhibition was determined for the most potent MAO B inhibitor. Docking poses and pharmacophore models were generated to confirm the in vitro results.

Results

N-(2,4-Dinitrophenyl)benzo[d][1,3

SUBMITTER: Hagenow J 

PROVIDER: S-EPMC6996489 | biostudies-literature | 2020

REPOSITORIES: biostudies-literature