Potent and selective isophthalamide S₂ hydroxyethylamine inhibitors of BACE1

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• 作者：Steven W. Kortum ; Timothy E. Benson ; Michael J. Bienkowski ; Thomas L. Emmons ; D. Bryan Prince ; Donna J. Paddock ; Alfredo G. Tomasselli ; Joseph B. Moon ; Alice LaBorde ; Ruth E. TenBrink
• 关键词：BACE1 ; Isophthalamide ; HEA ; Alzheimer’ ; s disease ; Hydroxyethylamine ; Inhibitor ; S2 pocket ; β ; -Secretase
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2007
• 出版时间：15 June 2007
• 年：2007
• 卷：17
• 期：12
• 页码：3378-3383
• 全文大小：219 K

文摘

The design and synthesis of a novel series of potent BACE1 hydroxyethylamine inhibitors. These inhibitors feature hydrogen bonding substituents at the C-5 position of the isophthalamide ring with improved selectivity over cathepsin D.