Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 17, Issue 19, Pages 6937-6941Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2009.08.017
Keywords
Alzheimer's disease; Hupzine A; AChE; Docking study
Funding
- Program of Promoting Development for Guizhou, China [Qian-01-2005-01]
- CAS
- National Sciences of Yunnan, China [2005C0010Z]
- Chinese Academy of Sciences [KSCX2-YW-G-038]
- National Natural Science Foundation of China [30772636]
Ask authors/readers for more resources
By targeting multi-active sites of acetylcholinesterase (AChE), a series of huperzine A (Hup A) derivatives with various aromatic ring groups were designed and synthesized by Schiff reaction. They were evaluated as AChE and butyrylcholinesterase (BChE) inhibitors. Results showed very significant specificity that the group of imine derivatives could inhibit TcAChE and hAChE, but no inhibitory effect on hBChE was detected. The experiment was explained by a docking study. In the docking model, we confirmed that aromatic ring of Hup A derivatives played the pi-pi stacking against aminophenol residues of AChE, and the structure-activity relationship (SAR) was discussed. (C) 2009 Elsevier Ltd. All rights reserved.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available