Inhibition of cholinesterase activity and amyloid aggregation by berberine-phenyl-benzoheterocyclic and tacrine-phenyl-benzoheterocyclic hybrids
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Add time:07/13/2019 Source:sciencedirect.com
A series of berberine-phenyl-benzoheterocyclic (26–29) and tacrine-phenyl-benzoheterocyclic hybrids (44–46) were synthesised and evaluated as multifunctional anti-Alzheimer’s disease agents. Compound 44b, tacrine linked with phenyl-benzothiazole by 3-carbon spacers, was the most potent AChE inhibitor with an IC50 value of 0.017 μM. This compound demonstrated similar Aβ aggregation inhibitory activity with cucurmin (51.8% vs 52.1% at 20 μM, respectively), indicating that this hybrid is an excellent multifunctional drug candidate for AD.
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