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 ,
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.
