期刊
MEDICINAL CHEMISTRY RESEARCH
卷 25, 期 9, 页码 2005-2014出版社
SPRINGER BIRKHAUSER
DOI: 10.1007/s00044-016-1648-1
关键词
Alzheimer's disease; 1H-Benzimidazole; Acetylcholinesterase inhibitor; Butyrylcholinesterase inhibitor; Ellman's method; Molecular modeling
资金
- TUBITAK (Turkish Scientific and Technical Research Council) [213S027]
A series of N-{2-[2-(1H-benzimidazole-2-yl)phenoxy]ethyl} substituted amine derivatives were synthesized and tested for their cholinesterase inhibitor activity. Acetylcholinesterase and butyrylcholinesterase inhibitor activities were evaluated in vitro by using Ellman's method. According to the activity results, all of the compounds displayed moderate acetylcholinesterase inhibitory activity and most of the compounds displayed remarkable butyrylcholinesterase inhibitory activity. Compound 3d was the most active compound in the series and also a selective butyrylcholinesterase inhibitor. Molecular docking studies and molecular dynamic simulations were also carried out.
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