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

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.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Choi JW,Jang BK,Cho NC,Park JH,Yeon SK,Ju EJ,Lee YS,Han G,Pae AN,Kim DJ,Park KD

doi

10.1016/j.bmc.2015.08.012

subject

Has Abstract

pub_date

2015-10-01 00:00:00

pages

6486-96

issue

19

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(15)00679-3

journal_volume

23

pub_type

杂志文章

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