期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 27, 期 2, 页码 232-236出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2016.11.067
关键词
Alzheimer's disease; Amyloid beta; Cholinesterase inhibition; Antioxidant; beta-Carbolines
资金
- University of Massachusetts Boston
- National Institute of Health [R21AG028816-01]
The design, synthesis and assessment of beta-carboline core-based compounds as potential multifunctional agents against several processes that are believed to play a significant role in Alzheimer's disease (AD) pathology, are described. The activity of the compounds was determined in A beta self-assembly (fibril and oligomer formation) and cholinesterase (AChE, BuChE) activity inhibition, and their antioxidant properties were also assessed. To obtain insight into the mode of action of the compounds, HR-MS studies were carried out on the inhibitor-A beta complex formation and molecular docking was performed on inhibitor-BuChE interactions. While several compounds exhibited strong activities in individual assays, compound 14 emerged as a promising multi-target lead for the further structure-activity relationship studies. (C) 2016 Elsevier Ltd. All rights reserved.
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