Conformationally biased P3 amide replacements of β-secretase inhibitors

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• 作者：Shawn J. Stachel ; Craig A. Coburn ; Thomas G. Steele ; Min-Chi Crouthamel ; Beth L. Pietrak ; Ming-Tain Lai ; M. Katharine Holloway ; Sanjeev K. Munshi ; Samuel L. Graham and Joseph P. Vacca
• 关键词：β ; -Secretase ; P3 ; Amide replacement
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2006
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：1 February 2006
• 卷：16
• 期：3
• 页码：641-644
• 文件大小：161 K

摘要

We have synthesized and evaluated a series of conformationally biased P3 amide replacements based on an isophthalamide lead structure. The studies resulted in the identification of the β-secretase inhibitor 7m which has an in vitro IC₅₀ = 35 nM. The synthesis and biological activities of these compounds are described.