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, ...
Related Articles:
Origin of the reactivity differences of substituted aziridines: CN vs CC bond breakages
[Kim, Yongeun; Kang, Lae-Sung; Ha, Hyun-Joon; Ko, Seung Whan; Lee, Won Koo Heterocycles, 2007 , vol. 71, # 10 p. 2243 - 2248]
Asymmetric synthesis of optically pure pharmacologically relevant amines employing ω??transaminases
[Advanced Synthesis and Catalysis, , vol. 350, # 17 p. 2761 - 2766]
Enzymatic enantiomeric resolution of phenylethylamines structurally related to amphetamine
[Organic and Biomolecular Chemistry, , vol. 9, # 23 p. 8171 - 8177]
Asymmetric synthesis of optically pure pharmacologically relevant amines employing ω??transaminases
[Advanced Synthesis and Catalysis, , vol. 350, # 17 p. 2761 - 2766]
An efficient enantioselective synthesis of (R, R)-formoterol, a potent bronchodilator, using lipases
[Tetrahedron Asymmetry, , vol. 11, # 13 p. 2705 - 2717]