Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 114, Issue -, Pages 162-169Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2016.02.038
Keywords
Monoamine oxidase; Neuroprotection; Drug design; Synthesis; Enzyme; Chalcones
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Funding
- Office of Academic Research, Qatar University, Doha, Qatar [QUST-CPH-FALL-14\-15-9, QUST-CPH-SPR-14/15-9]
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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 K-i values in the micromolar to sub-micromolar range. Molecular modeling studies have been performed to get insight into the binding mode of the synthesized compounds to human MAO-B active site. (C) 2016 Elsevier Masson SAS. All rights reserved.
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