Inhibition of Monoamine Oxidases by Pyridazinobenzylpiperidine Derivatives.

ABSTRACT: Monoamine oxidase inhibitors (MAOIs) have been crucial in the search for anti-neurodegenerative medications and continued to be a vital source of molecular and mechanistic diversity. Therefore, the search for selective MAOIs is one of the main areas of current drug development. To increase the effectiveness and safety of treating Parkinson's disease, new scaffolds for reversible MAO-B inhibitors are being developed. A total of 24 pyridazinobenzylpiperidine derivatives were synthesized and evaluated for MAO. Most of the compounds showed a higher inhibition of MAO-B than of MAO-A. Compound S5 most potently inhibited MAO-B with an IC₅₀ value of 0.203 μM, followed by S16 (IC₅₀ = 0.979 μM). In contrast, all compounds showed weak MAO-A inhibition. Among them,

SUBMITTER: Oh JM 

PROVIDER: S-EPMC11243598 | biostudies-literature | 2024 Jun

REPOSITORIES: biostudies-literature