Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 23, Issue 9, Pages 1963-1974Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2015.03.034
Keywords
Alzheimer's disease; beta-Secretase; BACE1 inhibitor; Synthesis; Docking
Funding
- 12th Fudan University Graduates Innovation Project, National Natural Science Foundation of China [81172975, 81001392]
- National High Technology Research and Development Program of China (863 Program) [2013AA092903]
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Nineteen new derivatives based on the structure of marine natural product tasiamide B were designed, synthesized, and evaluated for their inhibitory activity against BACE1, a potential therapeutic target for Alzheimer's disease. The hydrophobic substituents Val at P-3 position, Leu at P-1' position, Ala at P-2' position, and Phe at P-3' position were found to significantly affect the inhibition. Free carboxylic acid at C-terminus was also found to be important to the activity. In addition, the structure-activity relationships (SARs) were supported by molecular docking simulation. (C) 2015 Published by Elsevier Ltd.
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