2. Academic Validation
  3. Design and synthesis of novel chalcones as potent selective monoamine oxidase-B inhibitors

Design and synthesis of novel chalcones as potent selective monoamine oxidase-B inhibitors

  • Eur J Med Chem. 2016 May 23;114:162-9. doi: 10.1016/j.ejmech.2016.02.038.
Arwa Hammuda 1,  Raed Shalaby 1,  Stefano Rovida 2,  Dale E Edmondson 3,  Claudia Binda 2,  Ashraf Khalil 4
Affiliations

Affiliations

  • 1 College of Pharmacy, Qatar University, Doha, Qatar.
  • 2 Department of Biology and Biotechnology, University of Pavia, Via Ferrata 1, 27100, Pavia, Italy.
  • 3 Department of Biochemistry, Emory University School of Medicine, Atlanta, GA, 30322, USA.
  • 4 College of Pharmacy, Qatar University, Doha, Qatar. Electronic address: akhalil@qu.edu.qa.
PMID: 26974383 DOI: 10.1016/j.ejmech.2016.02.038
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.

Keywords

Chalcones; Drug design; Enzyme; Monoamine oxidase; Neuroprotection; Synthesis.

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