Trimethoxylated Halogenated Chalcones as Dual Inhibitors of MAO-B and BACE-1 for the Treatment of Neurodegenerative Disorders.

ABSTRACT: Six halogenated trimethoxy chalcone derivatives (CH1-CH6) were synthesized and spectrally characterized. The compounds were further evaluated for their inhibitory potential against monoamine oxidases (MAOs) and β-secretase (BACE-1). Six compounds inhibited MAO-B more effectively than MAO-A, and the 2',3',4'-methoxy moiety in CH4-CH6 was more effective for MAO-B inhibition than the 2',4',6'-methoxy moiety in CH1-CH3. Compound CH5 most potently inhibited MAO-B, with an IC₅₀ value of 0.46 µM, followed by CH4 (IC₅₀ = 0.84 µM). In 2',3',4'-methoxy derivatives (CH4-CH6), the order of inhibition was -Br in CH5 > -Cl in CH4 > -F in CH6 at the para-position in ring B of chalcone. CH4 and CH5 were selective for MAO-B, with selectivity index (SI) values of 15.1 and 31.3,

SUBMITTER: Vishal PK 

PROVIDER: S-EPMC8226672 | biostudies-literature | 2021 Jun

REPOSITORIES: biostudies-literature