Inhibition of cholinesterase activity and amyloid aggregation by berberine-phenyl-benzoheterocyclic and tacrine-phenyl-benzoheterocyclic hybrids

L Huang, T Su, W Shan, Z Luo, Y Sun, F He…

Index: Huang, Ling; Su, Tao; Shan, Wenjun; Luo, Zonghua; Sun, Yang; He, Feng; Li, Xingshu Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 9 p. 3038 - 3048

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Citation Number: 29

Abstract

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% ...