A novel series of tacrine–selegiline hybrids with cholinesterase and monoamine oxidase inhibition activities for the treatment of Alzheimer's disease

C Lu, Q Zhou, J Yan, Z Du, L Huang, X Li

Index: Lu, Chuanjun; Zhou, Qi; Yan, Jun; Du, Zhiyun; Huang, Ling; Li, Xingshu European Journal of Medicinal Chemistry, 2013 , vol. 62, p. 745 - 753

Full Text: HTML

Citation Number: 35

Abstract

A novel series of tacrine–selegiline hybrids was synthesised and evaluated for application as inhibitors of cholinesterase (AChE/BuChE) and monoamine oxidase (MAO-A/B). The results demonstrate that most of the synthesised compounds exhibit high inhibitory activity. Among these compounds, compound 8g provided a good balance of activity towards all targets (with IC50 values of 22.6 nM, 9.37 nM, 0.3724 μM, and 0.1810 μM for AChE, ...