Bioorganic & Medicinal Chemistry 2013-12-01

Inhibition of cholinesterase and monoamine oxidase-B activity by Tacrine–Homoisoflavonoid hybrids

Yang Sun, Jianwen Chen, Xuemin Chen, Ling Huang, Xingshu Li

Index: Bioorg. Med. Chem. 21(23) , 7406-17, (2013)

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Abstract

A series of Tacrine–Homoisoflavonoid hybrids were designed, synthesised, and evaluated as inhibitors of cholinesterases (ChEs) and human monoamine oxidases (MAOs). Among these hybrids, compound 8b were observed to be potent inhibitors of AChE and MAO-B, with IC50 values of 67.9nM and 0.401μM, respectively. The PAMPA-BBB assay also demonstrated that this compound has the ability to cross the BBB (blood–brain barrier).