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

Publication Type : Journal Article

Publisher : Comb Chem High Throughput Screen

Source : Comb Chem High Throughput Screen, Volume 20, Issue 6, p.522-532 (2017)

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Keywords : Chromones, Dose-Response Relationship, Drug, High-Throughput Screening Assays, Humans, Molecular Structure, Monoamine oxidase, Monoamine Oxidase Inhibitors, Structure-Activity Relationship

Campus : Kochi

School : School of Pharmacy

Center : Amrita Institute of Medical Science

Department : Pharmaceutical Chemistry & Analysis

Year : 2017

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.

Cite this Research Publication : Bijo Mathew, Mathew, G. Elizabeth, Petzer, J. P., and Petzer, A., “Structural Exploration of Synthetic Chromones as Selective MAO-B Inhibitors: A Mini Review.”, Comb Chem High Throughput Screen, vol. 20, no. 6, pp. 522-532, 2017.

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