Melatonin Analogues Potently Inhibit MAO-B and Protect PC12 Cells against Oxidative Stress.

ABSTRACT: Monoamine oxidase B (MAO-B) metabolizes dopamine and plays an important role in oxidative stress by altering the redox state of neuronal and glial cells. MAO-B inhibitors are a promising therapeutical approach for Parkinson's disease (PD). Herein, 24 melatonin analogues (3a-x) were synthesized as novel MAO-B inhibitors with the potential to counteract oxidative stress in neuronal PC12 cells. Structure elucidation, characterization, and purity of the synthesized compounds were performed using ¹H-NMR, ¹³C-NMR, HRMS, and HPLC. At 10 µM, 12 compounds showed >50% MAO-B inhibition. Among them, compounds 3n, 3r, and 3u-w showed >70% inhibition of MAO-B and IC₅₀ values of 1.41, 0.91, 1.20, 0.66, and 2.41 µM, respectively. W

SUBMITTER: Elkamhawy A 

PROVIDER: S-EPMC8533333 | biostudies-literature | 2021 Oct

REPOSITORIES: biostudies-literature