Journal
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
Volume 24, Issue 2, Pages 372-380Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1080/14756360802187885
Keywords
Alzheimer's disease; acetylcholinesterase; inhibitors; flavonoids; benzylpiperidine
Funding
- National Natural Science Foundation of China [30572239]
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A new series of flavonoid derivatives have been designed, synthesised and evaluated as acetylcholinesterase inhibitors that could bind simultaneously to the peripheral and catalytic sites of the enzyme. Among them, fifteen derivatives were found to inhibit the enzyme in the micromolar range and isoflavone derivatives possessed more potent inhibitory activity than other flavonoid derivatives. The best compound 9a had its inhibitory activity (IC50=0.093M) in the same range as the reference compound, donepezil (IC50=0.025M). Preliminary structure-activity relationships and a molecular modeling study for 9a have revealed that the isoflavone moiety plays a key role in the interaction of this series of derivatives with AChE by acting as an anchor in its peripheral anionic site.
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