4- Substituted sampangine derivatives: Novel acetylcholinesterase and β-myloid aggregation inhibitors.

Abstract:

:A series of 4- substituted sampangine derivatives (4-aminoalkylaminosampangine Ar-NH(CH2)nNR1R2) has been designed, synthesized, and tested for their ability to inhibit acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and β-myloid (Aβ) aggregation. The synthetic compounds exhibited high AChE inhibitory activity and a significant in vitro inhibitory potency toward the self-induced Aβ aggregation. While, treatment of SH-SY5Y cells overexpressing the Swedish mutant form of human β-amyloid precursor protein (APPsw) with derivatives was associated with significant reduction of Aβ42 secretion levels. Moreover, most of the synthetic compounds were predicted to be able to cross the blood-brain barrier (BBB) to reach their targets in the central nervous system (CNS) according to a parallel artificial membrane permeation assay for BBB. The result encourages us to study this class of compounds thoroughly and systematically.

journal_name

Int J Biol Macromol

authors

Chen KL,Gan L,Wu ZH,Qin JF,Liao WX,Tang H

doi

10.1016/j.ijbiomac.2017.10.157

subject

Has Abstract

pub_date

2018-02-01 00:00:00

pages

2725-2729

issue

Pt B

eissn

0141-8130

issn

1879-0003

pii

S0141-8130(17)32978-1

journal_volume

107

pub_type

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