Abstract
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.
Combinatorial Chemistry & High Throughput Screening
Title:Structural Exploration of Synthetic Chromones as Selective MAO-B Inhibitors: A Mini Review
Volume: 20 Issue: 6
Author(s): Bijo Mathew*, Githa Elizabeth Mathew, Jacobus P. Petzer and Anel Petzer
Affiliation:
- Division of Drug Design and Medicinal Chemistry Research Lab, Department of Pharmaceutical Chemistry, Ahalia School of Pharmacy, Palakkad 678557, Kerala,India
Keywords: Monoamine oxidase, chromone, coumarin, chalcone, reversible inhibition, Parkinson's disease.
Abstract: 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.
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Cite this article as:
Mathew Bijo*, Mathew Elizabeth Githa, Petzer P. Jacobus and Petzer Anel, Structural Exploration of Synthetic Chromones as Selective MAO-B Inhibitors: A Mini Review, Combinatorial Chemistry & High Throughput Screening 2017; 20 (6) . https://dx.doi.org/10.2174/1386207320666170227155517
DOI https://dx.doi.org/10.2174/1386207320666170227155517 |
Print ISSN 1386-2073 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5402 |
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