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  • Title: Design and synthesis of novel chalcones as potent selective monoamine oxidase-B inhibitors.
    Author: Hammuda A, Shalaby R, Rovida S, Edmondson DE, Binda C, Khalil A.
    Journal: Eur J Med Chem; 2016 May 23; 114():162-9. PubMed ID: 26974383.
    Abstract:
    A novel series of substituted chalcones were designed and synthesized to be evaluated as selective human MAO-B inhibitors. A combination of either methylsulfonyl or trifluoromethyl substituents on the aromatic ketone moiety with a benzodioxol ring on the other end of the chalcone scaffold was investigated. The compounds were tested for their inhibitory activities on both human MAO-A and B. All compounds appeared to be selective MAO-B inhibitors with Ki values in the micromolar to submicromolar range. Molecular modeling studies have been performed to get insight into the binding mode of the synthesized compounds to human MAO-B active site.
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