Multifunctional tacrine–flavonoid hybrids with cholinergic, β-amyloid-reducing, and metal chelating properties for the treatment of Alzheimer's disease

…, XB Wang, SS Xie, N Jiang, KDG Wang, HQ Yao…

Index: Li, Su-Yi; Wang, Xiao-Bing; Xie, Sai-Sai; Jiang, Neng; Wang, Kelvin D.G.; Yao, He-Quan; Sun, Hong-Bin; Kong, Ling-Yi European Journal of Medicinal Chemistry, 2013 , vol. 69, p. 632 - 646

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Citation Number: 23

Abstract

Abstract A new series of tacrine–flavonoid hybrids (13a–u) had been designed, synthesized, and evaluated as multifunctional cholinesterase (ChE) inhibitors against Alzheimer's disease (AD). In vitro studies showed that most of the molecules exhibited a significant ability to inhibit ChE and self-induced amyloid-β (Aβ 1–42) aggregation. Kinetic and molecular modeling studies also indicated compounds were mixed-type inhibitors, ...