Title of article
Conformationally biased P3 amide replacements of β-secretase inhibitors
Author/Authors
Shawn J. Stachel، نويسنده , , Craig A. Coburn، نويسنده , , Thomas G. Steele، نويسنده , , Min-Chi Crouthamel، نويسنده , , Beth L. Pietrak، نويسنده , , Ming-Tain Lai، نويسنده , , M. Katharine Holloway، نويسنده , , Sanjeev K. Munshi، نويسنده , , Samuel L. Graham، نويسنده , , Joseph P. Vacca، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
4
From page
641
To page
644
Abstract
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.
Keywords
?-Secretase , Amide replacement , P3
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
796431
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