Synthesis and biological evaluation of berberine–thiophenyl hybrids as multi-functional agents: Inhibition of acetylcholinesterase, butyrylcholinesterase, and Aβ …

T Su, S Xie, H Wei, J Yan, L Huang, X Li - Bioorganic & medicinal chemistry, 2013 - Elsevier
A series of berberine–thiophenyl hybrids were designed, synthesised, and evaluated as
inhibitors of acetylcholinesterase (AChE), butyrylcholinesterase (BuChE) and β-amyloid (Aβ)
aggregation and as antioxidants. Among these hybrids, compounds 4f and 4i, berberine
linked with o-methylthiophenyl and o-chlorothiophenyl by a 2-carbon spacer, were observed
to be potent inhibitors of AChE, with IC 50 values of 0.077 and 0.042 μM, respectively. Of the
tested compounds, 4i was also the most potent inhibitor of BuChE, with an IC 50 value of …
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