Journal
MOLECULES
Volume 25, Issue 18, Pages -Publisher
MDPI
DOI: 10.3390/molecules25184064
Keywords
in silico; in vitro; QSAR; docking; flavone; acetylcholinesterase; beta-secretase
Funding
- Vietnam National Foundation for Science and Technology Development (NAFOSTED) [106-YS.05-2015.31]
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Acetylcholinesterase (AChE) and beta-secretase (BACE-1) have become attractive therapeutic targets for Alzheimer's disease (AD). Flavones are flavonoid derivatives with various bioactive effects, including AChE and BACE-1 inhibition. In the present work, a series of 14 flavone derivatives was synthesized in relatively high yields (35-85%). Six of the synthetic flavones (B4, B5, B6, B8, D6 and D7) had completely new structures. The AChE and BACE-1 inhibitory activities were tested, giving pIC(50) 3.47-4.59 (AChE) and 4.15-5.80 (BACE-1). Three compounds (B3, D5 and D6) exhibited the highest biological effects on both AChE and BACE-1. A molecular docking investigation was conducted to explain the experimental results. These molecules could be employed for further studies to discover new structures with dual action on both AChE and BACE-1 that could serve as novel therapies for AD.
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