期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 128, 期 -, 页码 237-246出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2017.01.042
关键词
Acetylcholinesterase; Butyrylcholinesterase; Alzheimer's disease; Tacrine
资金
- Research Council of Tehran University of Medical Sciences [95-03-92-33171]
- Iran National Science Foundation (INSF)
A series of poly-functionalized tacrine-derived compounds namely 5-amino-2-phenyl-4H-pyrano[2,3-b] quinoline-3-carboxylates were designed and synthesized as cholinesterases inhibitors. The in vitro inhibition assay against AChE and BuChE demonstrated that most of compounds had potent AChE inhibitory with reserving potential of BuChE inhibition. Among them, compound 6i bearing a 4-(3-bromophenyl) moiety showed the most potent activity against AChE/BuChE (IC(50)s values of 0.069 and 1.35 mu M, respectively). The anti-AChE activity of 6i was five times more than that of tacrine. The SAR study revealed that chloro/bromo substituent at ortho or meta position of the 4-phenyl ring can improve the anticholinesterase activity. (C) 2017 Elsevier Masson SAS. All rights reserved.
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