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

被引：94

作者：

Lu, Chuanjun ^{[1
]}

Zhou, Qi ^{[1
]}

Yan, Jun ^{[1
]}

Du, Zhiyun ^{[2
]}

Huang, Ling ^{[1
]}

Li, Xingshu ^{[1
]}

机构：

[1] Sun Yat Sen Univ, Sch Pharmaceut Sci, Inst Drug Synth & Pharmaceut Proc, Guangzhou 510006, Guangdong, Peoples R China

[2] Guang Dong Univ Technol, Fac Light Ind & Chem Engn, Guangzhou 510006, Guangdong, Peoples R China

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2013年 / 62卷

关键词：

Tacrine; Selegiline; Cholinesterase inhibitor; Monoamine oxidase inhibitor; Alzheimer's disease; BIOLOGICAL EVALUATION; ACETYLCHOLINESTERASE INHIBITORS; DERIVATIVES; BUTYRYLCHOLINESTERASE; POTENT; PEPTIDE; AGENTS; ALKYL; MAO;

D O I：

10.1016/j.ejmech.2013.01.039

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 mu M, and 0.1810 mu M for AChE, BuChE, MAO-A and MAO-B, respectively). These results indicated that 8g has the potential to be a multi-functional candidate for Alzheimer's disease. (C) 2013 Elsevier Masson SAS. All rights reserved.

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收藏

页码：745 / 753

页数：9

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