Design, synthesis, biological evaluation and docking study of 5-oxo-4,5-dihydropyrano[3,2-c]chromene derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors
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- 作者：Mehdi Khoobi ; Masoumeh Alipour ; Amirhossein Sakhteman ; Hamid Nadri ; Alireza Moradi ; Mehdi Gh ; i ; Saeed Emami ; Alireza Foroumadi ; Abbas Shafiee
- 关键词：Alzheimer's disease ; Acetylcholinesterase ; Chromenes ; Coumarins ; Docking study
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2013
- 出版时间：October, 2013
- 年：2013
- 卷：68
- 期：Complete
- 页码：260-269
- 全文大小：1805 K
文摘
A series of fused coumarins namely 5-oxo-4,5-dihydropyrano[3,2-c]chromenes linked to N-benzylpyridinium scaffold were synthesized and evaluated as acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitors. The 1-(4-fluorobenzyl)pyridinium derivative 6g showed the most potent anti-AChE activity (IC50 value?=?0.038?¦ÌM) and the highest AChE/BuChE selectivity (SI?>?48). The docking study permitted us to rationalize the observed structure-affinity relationships and to detect possible binding modes.