Synthesis of a series of unsaturated ketone derivatives as selective and reversible monoamine oxidase inhibitors

Title
Synthesis of a series of unsaturated ketone derivatives as selective and reversible monoamine oxidase inhibitors
Authors
최지원장보고조남철박종현연슬기주은지이용섭한균희배애님김동진박기덕
Keywords
a,b-Unsaturated carbonyl derivatives; Chalcone; Monoamine oxidase; MAO-B inhibitor; Reversible inhibitor
Issue Date
2015-10
Publisher
Bioorganic & medicinal chemistry
Citation
VOL 23, 6486-6496
Abstract
We have synthesized three categories of α,β-unsaturated carbonyl derivatives and evaluated their MAO-A and MAO-B inhibitory activities. Among them, compound 10b including α,β-unsaturated ketone group showed the most potent and selective MAO-B inhibitory activity (IC50 human MAO-B 16 nM, >6000-fold selective vs MAO-A) and compound 10b exhibited good reversibility compared with selegiline, a well-known irreversible MAO-B inhibitor. However, both α,β-unsaturated amide and ester derivatives exhibited weaker MAO-B inhibition potencies. The docking studies provided insights into the possible binding modes and the key interaction sites of the synthesized MAO-B inhibitors.
URI
http://pubs.kist.re.kr/handle/201004/50299
ISSN
09680896
Appears in Collections:
KIST Publication > Article
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