The evaluation of 1-tetralone and 4-chromanone derivatives as inhibitors of monoamine oxidase.

ABSTRACT: Monoamine oxidase (MAO) is of much clinical relevance, and inhibitors of this enzyme are used in the treatment for neuropsychiatric and neurodegenerative disorders such as depression and Parkinson's disease. The present study synthesises and evaluates the MAO inhibition properties of a series of 33 1-tetralone and 4-chromanone derivatives in an attempt to discover high-potency compounds and to expand on the structure-activity relationships of MAO inhibition by these classes. Among these series, eight submicromolar MAO-A inhibitors and 28 submicromolar MAO-B inhibitors are reported, with all compounds acting as specific inhibitors of the MAO-B isoform. The most potent inhibitor was a 1-tetralone derivative (1h) with IC₅₀ values of 0.036 and 0.0011 µM for MAO-A and MAO-B, respecti

SUBMITTER: Cloete SJ 

PROVIDER: S-EPMC7512223 | biostudies-literature | 2021 Feb

REPOSITORIES: biostudies-literature