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Trimethoxylated Halogenated Chalcones as Dual Inhibitors of MAO-B and BACE-1 for the Treatment of Neurodegenerative Disorders by Vishal, Vishal Payyalot (author);Oh, Jong Min (author);Khames, Ahmed (author);Abdelgawad, Mohamed A. (author);Nair, Aathira Sujathan (author);Nath, Lekshmi R. (author);Gambacorta, Nicola (author);Ciriaco, Fulvio (author);Nicolotti, Orazio (author);Kim, Hoon (author);Mathew, Bijo (author) is a Pharmacology, Toxicology and Pharmaceutics article available to read on EtoBox.

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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, respectively, over MAO-A. CH4 and CH5 moderately inhibited BACE-1 with IC50 values of 13.6 and 19.8 μM, respectively. When CH4 and CH5 were assessed for their cell viability studies on the normal African Green Monkey kidney cell line (VERO) using MTT assays, it was noted that both compounds were found to be safe, and only a slightly toxic effect was observed in concentrations above 200 μg/mL. CH4 and CH5 decreased reactive ox

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Author

Vishal, Vishal Payyalot (author);Oh, Jong Min (author);Khames, Ahmed (author);Abdelgawad, Mohamed A. (author);Nair, Aathira Sujathan (author);Nath, Lekshmi R. (author);Gambacorta, Nicola (author);Ciriaco, Fulvio (author);Nicolotti, Orazio (author);Kim, Hoon (author);Mathew, Bijo (author)

Publisher

MDPI AG

Published

2021

Language

EN

Field

Pharmacology, Toxicology and Pharmaceutics (Life Sciences)