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哌啶嵌入新型五环笼状化合物的简便合成及其抗乙酰胆碱酯酶活性筛选

An expedient synthesis and screening for antiacetylcholinesterase activity of piperidine embedded novel pentacyclic cage compounds.

作者信息

Kumar Raju Suresh, Almansour Abdulrahman I, Arumugam Natarajan, Osman Hasnah, Ali Mohamed Ashraf, Basiri Alireza, Kia Yalda

机构信息

Department of Chemistry, College of Sciences, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia.

出版信息

Med Chem. 2014 Mar;10(2):228-36. doi: 10.2174/157340641002140131170054.

DOI:10.2174/157340641002140131170054
PMID:23627271
Abstract

The aim of this study was to synthesize and evaluate diazapentacyclic analogs for their acetylcholinesterase (AChE) inhibitory activity. The pentacyclic analogs were synthesized by one-pot three-component domino reactions in a microwave synthesizer. Most of the compounds exhibited moderate to good AChE inhibitory activity, compound 5i showed potent inhibitory activity with IC50 1.12 ± 0.01 µM and this may provide a new lead for developing potential inhibitors for Alzheimer's disease.

摘要

本研究的目的是合成并评估二氮杂五环类似物的乙酰胆碱酯酶（AChE）抑制活性。通过在微波合成仪中进行一锅三组分多米诺反应合成了五环类似物。大多数化合物表现出中度至良好的AChE抑制活性，化合物5i表现出强效抑制活性，IC50为1.12±0.01μM，这可能为开发阿尔茨海默病的潜在抑制剂提供新的先导化合物。

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