Development of Isopropyl-Tailed Chalcones as a New Class of Selective MAO-B Inhibitors for the Treatment of Parkinson's Disorder.

ABSTRACT: Thirteen isopropyl chalcones (CA1-CA13) were synthesized and evaluated for their inhibitory activity against monoamine oxidase (MAO). All compounds inhibited MAO-B more effectively than MAO-A. Compound CA4 most potently inhibited MAO-B with an IC₅₀ value of 0.032 μM, similar to that of CA3 (IC₅₀ = 0.035 μM) and with high selectivity index (SI) values for MAO-B over MAO-A (SI = 49.75 and 353.23, respectively). The -OH (CA4) or -F (CA3) group at the para position on the A ring provided higher MAO-B inhibition than that of the other substituents (-OH ≥ -F > -Cl > -Br > -OCH₂CH₃ > -CF₃). On the other hand, compound CA10 most potently inhibited MAO-A with an IC₅₀ value of 0.310 μM and eff

SUBMITTER: Kumar S 

PROVIDER: S-EPMC9947953 | biostudies-literature | 2023 Feb

REPOSITORIES: biostudies-literature