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Combinatorial Chemistry & High Throughput Screening

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ISSN (Print): 1386-2073
ISSN (Online): 1875-5402

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Review Article

Flavonoid and Chalcone Scaffolds as Inhibitors of BACE1: Recent Updates

Author(s): Anishma Payyappilliparambil Narayanan, Jayalakshmi Jayan, Sachithra Thazhathuveedu Sudevan, Archana Dhyani, Subin Mary Zachariah* and Bijo Mathew*

Volume 27, Issue 9, 2024

Published on: 26 September, 2023

Page: [1243 - 1256] Pages: 14

DOI: 10.2174/1386207326666230731092409

Price: $65

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Abstract

Flavonoids and chalcones are two major classes of chemical moieties that have a vast background of pharmacological activities. Chalcone is a subclass of flavonoids whose therapeutic potential has been implicated due to an array of bioactivities. A lot of research works have shown interest in investigating the neuroprotective effect of these molecules, and have revealed them to be much more potent molecules that can be used to treat neurodegenerative disorders. Beta-site APP cleaving enzyme (BACE1), which is majorly found in the brain, is one of the reasons behind the development of Alzheimer’s disease (AD). Flavonoids and chalcones have proven clinical data that they inhibit the production of Aβ plaques that are involved in the progression of AD. In this article, we have provided a detailed chronological review of the research work on the BACE1 inhibiting potency of both flavonoids and chalcones. Almost all the flavonoids and chalcones mentioned in this article have shown very good in vitro and in vivo BACE1 inhibiting activity. The docking studies and the structural importance of some BACE1-inhibiting flavonoids, as well as chalcones, are also mentioned here.

Keywords: BACE1 inhibitors, Aβ plagues, AD, flavonoids, chalcones, inhibitors.

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