ArticlePharmaceuticals (Basel, Switzerland)2022
Development of Halogenated-Chalcones Bearing with Dimethoxy Phenyl Head as Monoamine Oxidase-B Inhibitors.
Article in Pharmaceuticals (Basel, Switzerland), 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed, 18 citations in OpenAlex.
- Inhibition of monoamine oxidase by fluorobenzyloxy chalcone derivatives.RSC advances · 2025Article
- Monoamine Oxidase Inhibitors in Drug Discovery Against Parkinson's Disease: An Update.Pharmaceuticals (Basel, Switzerland) · 2025Review
- MAO-B Inhibitor (2E)-3-(4-Bromophenyl)-1-(1H-indol-3-yl) prop-2-en-1-one as a Neuroprotective Agent Against Alzheimer's Disease.Neurochemical research · 2024Article
- Recent updates on structural insights of MAO-B inhibitors: a review on target-based approach.Molecular diversity · 2024Review
- Drug Development for Alzheimer's and Parkinson's Disease: Where Do We Go Now?Pharmaceutics · 2024Review
- Isatin-tethered halogen-containing acylhydrazone derivatives as monoamine oxidase inhibitor with neuroprotective effect.Scientific reports · 2024Article
- New Insights on the Activity and Selectivity of MAO-B Inhibitors through In Silico Methods.International journal of molecular sciences · 2023Article
- Development of Isopropyl-Tailed Chalcones as a New Class of Selective MAO-B Inhibitors for the Treatment of Parkinson's Disorder.ACS omega · 2023Article
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Authors and funding
10 authors at 7 institutions in 5 countries.
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Abstract
Two series of dimethoxy-halogenated chalcones (DM1−DM20) were synthesized and tested for their ability to inhibit monoamine oxidase (MAOs). Compound DM2 exhibited the most significant inhibition against MAO-B with an IC50 value of 0.067 µM, followed by compound DM18 (IC50 = 0.118 µM), with selectivity index (SI) values of 93.88 and >338.98, respectively. However, none of the substances successfully inhibited MAO-A. The MAO-B inhibitors DM2 and DM18 were competitive and reversible, with Ki values of 0.032 ± 0.004 and 0.045 ± 0.001 µM, respectively. DM2 was non-toxic below 100 µg/mL in the cytotoxic test using the Vero epithelial cell line by the MTT method. According to molecular docking studies, DM2 and DM18 formed very similar conformations within the MAO-B binding pocket, with the ortho-chlorine and ortho-fluorine aromatic rings sandwiched between F168 and Y326. These conformations were predicted to show better interactions with the targeted MAO-B than MAO-A. In particular, the induced-fit docking of the dimethoxy phenyl ring of DM2 facing the hydrophobic pocket made up of FAD, Y398, and Y435 had an impact on F168 in the docking pocket. Taken together, DM2 and DM18 may be suitable candidates for treating neurodegenerative conditions such as Parkinson’s disease.
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