Design, synthesis and biological evaluation of tasiamide B derivatives as BACE1 inhibitors
Jian Liu1, Wuyan Chen2, Yechun Xu2
1School of Pharmacy, Fudan University, 826 Zhangheng Road, Shanghai 201203, China.
Abstract:
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 P₃ position, Leu at P₁' position, Ala at P₂' position, and Phe at P₃' 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.
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