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Synthesis of furocoumarin-stilbene hybrids as potential multifunctional drugs against multiple biochemical targets associated with Alzheimer's disease.

Abstract：

:A series of furocoumarin-stilbene hybrids has been synthesized and evaluated in vitro for inhibitory effect against acetylcholinesterase (AChE), butyrylcholinestarase (BChE), β-secretase, cyclooxygenase-2 (COX-2), and lipoxygenase-5 (LOX-5) activities including free radical-scavenging properties. Among these hybrids, 8-(3,5-dimethoxyphenyl)-4-(3,5-dimethoxystyryl)furochromen-2-one 4h exhibited significant anticholinesterase activity and inhibitory effect against β-secretase, COX-2 and LOX-5 activities. 2,2-Diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity and an in vitro cell-based antioxidant activity assay involving lipopolysaccharide induced reactive oxygen species production revealed that 4h has capability of scavenging free radicals. Molecular docking into AChE, BChE, β-secretase, COX-2 and LOX-5 active sites has also been performed.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Agbo EN,Gildenhuys S,Choong YS,Mphahlele MJ,More GK

doi

10.1016/j.bioorg.2020.103997

subject

Has Abstract

pub_date

2020-08-01 00:00:00

pages

103997

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(20)31294-3

journal_volume

101

pub_type

杂志文章

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