期刊
CHEMICAL BIOLOGY & DRUG DESIGN
卷 89, 期 5, 页码 783-789出版社
WILEY
DOI: 10.1111/cbdd.12902
关键词
acetylcholinesterase; Alzheimer's disease; benzo[d]oxazol; docking study
资金
- Research Council of Tehran University of Medical Sciences [95-02-45-32579]
- Iran National Science Foundation (INSF)
A series of novel benzo[d]oxazole derivatives (6a-n) have been synthesized and biologically evaluated as potential inhibitors of acetylcholinesterases (AChE) and butyrylcholinesterase (BChE). The chemical structures of all final compounds were confirmed by spectroscopic methods. In vitro studies showed that most of the synthesized compounds are potent acetylcholinester ase and butyrylcholinesterase inhibitors. Among them, compounds 6a and 6j strongly inhibited AChE and BChE activities with IC50 values of 1.03-1.35 and 6.6-8.1 mu m, respectively. Docking studies also provided the binding modes of action and identified hydrophobic pi forces as the main interaction.
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