Please use this identifier to cite or link to this item: http://hdl.handle.net/10397/22077
Title: Derivatives of oxoisoaporphine alkaloids : a novel class of selective acetylcholinesterase inhibitors
Authors: Tang, H
Ning, FX
Wei, YB
Huang, SL
Huang, ZS
Chan, ASC
Gu, LQ
Keywords: Acetylcholinesterase inhibitors
Butyrylcholinesterase
Oxoisoaporphine alkaloids
Synthesis
Issue Date: 2007
Publisher: Pergamon Press
Source: Bioorganic & medicinal chemistry letters, 2007, v. 17, no. 13, p. 3765-3768 How to cite?
Journal: Bioorganic & medicinal chemistry letters 
Abstract: A series of 9-aminoalkanamido-1-azabenzanthrones derviatives (3a-i Ar-NHCO(CH 2) nNR 1R 2) and their quaternary methiodide salts (4a-g Ar-NHCO(CH 2) nN +(CH 3)R 1R 2I -) were designed and synthesized as acetylcholinesterase (AChE) or butyrylcholinesterase (BuChE) inhibitors. The synthetic compounds exhibited high AChE inhibitory activity with IC 50 values in the nanomolar range and high selectivity for AChE over BuChE (45- to 1980-fold). The structure-activity relationships (SARs) were discussed.
URI: http://hdl.handle.net/10397/22077
ISSN: 0960-894X
EISSN: 1464-3405
DOI: 10.1016/j.bmcl.2007.04.015
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