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Publication Type : Journal Article
Publisher : European Journal of Medicinal Chemistry
Source : European Journal of Medicinal Chemistry, Volume 205, p.112650 (2020)
Keywords : Chalcone, Monoamine oxidase, MTDL, Natural compounds, Neurodegenerative diseases, Selective MAO-B inhibitors
Campus : Kochi
School : School of Pharmacy
Department : Pharmaceutical Chemistry & Analysis
Year : 2020
Abstract : In the last years the continuous efforts in the development of novel and effective inhibitors of human monoamine oxidases (hMAOs) promoted the discovery of new agents able to effectively and selectively bound one of the two isoforms (hMAO-A and hMAO-B). However, the parent chalcone scaffold still covers an important role in hMAOs inhibition. In the present work, we focused our attention on the researches performed in the last five years, involving chalcones or compounds that can be correlated to them. We classified the chalcones into different groups depending on their structural characteristics or common molecular properties. In this regard, we also considered chalcones based on heterocycles and compounds endowed with scaffolds containing a masked chalcone motif. When structural attributes could not be used, we took advantage of enzymatic activity to arrange compounds in a group. We followed this approach for the multitarget agents. Finally, we also analysed the naturally occurring chalcones. All the sections were discussed exhaustively and the structure-activity relationship (SAR) analyses were sustained by means of detailed images describing the effects related to the substituents or structural changes.
Cite this Research Publication : P. Guglielmi, Bijo Mathew, Secci, D., and Carradori, S., “Chalcones: Unearthing their therapeutic possibility as monoamine oxidase B inhibitors”, European Journal of Medicinal Chemistry, vol. 205, p. 112650, 2020.