Structural Exploration of Synthetic Chromones as Selective MAO-B Inhibitors: A Mini Review

Author(s): Bijo Mathew*, Githa Elizabeth Mathew, Jacobus P. Petzer, Anel Petzer.

Journal Name: Combinatorial Chemistry & High Throughput Screening

Volume 20 , Issue 6 , 2017

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Aim and Objective: Specific inhibitors of monoamine oxidase (MAO)-B are considered useful therapeutic agents in targeting neurological disorders like Alzheimer's and Parkinson's diseases. Due to the academic challenge of designing new hMAO-B inhibitors and the possibility of discovering compounds with improved properties compared to existing MAO-B inhibitors, a number of research groups are searching for new classes of chemical compounds that may act as selective hMAO-B inhibitors.

Materials and Methods: Among these, chromone (4H-1-benzopyran-4-one) derivatives have recently emerged as a chemotype with specific and high potency MAO-B inhibition. Chromones are structurally related to a series of coumarins and chalcones, which are well-known inhibitors of MAO-B.

Results: The experimental evidence has demonstrated that most of the chromone skeleton derived compounds have shown potent, reversible and selective type of hMAO-B inhibitors.

Conclusion: The current review focuses on the MAO-B inhibitory properties of various synthetically derived chromones with specific emphasis on the structure-activity relationships and molecular recognition of MAO-B inhibition by this class. This review covers the recent updates present in the literature and will certainly provide a greater insight for the design and development of new class of potent chromone based selective MAO-B inhibitors.

Keywords: Monoamine oxidase, chromone, coumarin, chalcone, reversible inhibition, Parkinson's disease.

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Article Details

Year: 2017
Page: [522 - 532]
Pages: 11
DOI: 10.2174/1386207320666170227155517
Price: $58

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