Synthesis and γ-secretase activity of APP substrate-based hydroxyethylene dipeptide isosteres

A Nadin, AP Owens, JL Castro, T Harrison…

文献索引：Nadin, Alan; Owens, Andrew P.; Castro, Jose L.; Harrison, Timothy; Shearman, Mark S. Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 1 p. 37 - 41

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被引用次数: 27

摘要

Two new APP substrate-based hydroxyethylene isosteres (AT and VI) were prepared and their dipeptide conjugates shown not to inhibit the γ-secretase-mediated formation of either Aβ1-40 or Aβ1-42. The FG isostere and a des-hydroxy hydroxyethylene isostere also gave inactive compounds. Conversely, a number of compounds containing the intact substrate- unrelated Phe-Phe (FF) hydroxyethylene isostere were shown to be potent inhibitors ( ...