期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 22, 期 8, 页码 2885-2888出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.02.057
关键词
Indoles; beta-Carbolines; Quinolines; Acetylcholinesterase inhibitory activity; Alzheimer's disease
资金
- National Research Council of Thailand (NRCT)
- Center of Excellence for Innovation in Chemistry (PERCH-CIC), Commission on Higher Education, Ministry of Education
Acetylcholinesterase (AChE) inhibitory activity is one of the proposed targets for indole analogs. Simple indoles with substitution of methoxy, carboxy or hydroxy at the benzene ring showed a low percent of inhibitory activity in eel-AChE. Adding a side chain at the pyrrole ring, such as serotonin, beta-carbolines and quinolines (the bioisostere of indole), improved the inhibitory activity significantly. However, proper substitution and conformation of the ring were required for good binding. The result of inhibition in human-AChE of serotonin, beta-carbolines and quinolines showed similar profile as eel-AChE with lower magnitude. The data from molecular docking showed that they shared the same binding site as galantamine. (C) 2012 Published by Elsevier Ltd.
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