Synthesis of a series of unsaturated ketone derivatives as selective and reversible monoamine oxidase inhibitors
- Synthesis of a series of unsaturated ketone derivatives as selective and reversible monoamine oxidase inhibitors
- 최지원; 장보고; 조남철; 박종현; 연슬기; 주은지; 이용섭; 한균희; 배애님; 김동진; 박기덕
- a,b-Unsaturated carbonyl derivatives; Chalcone; Monoamine oxidase; MAO-B inhibitor; Reversible inhibitor
- Issue Date
- Bioorganic & medicinal chemistry
- VOL 23, 6486-6496
- 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.
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