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  • Conformationally biased P3 amide replacements of beta-secretase inhibitors.

Conformationally biased P3 amide replacements of beta-secretase inhibitors.

Bioorganic & medicinal chemistry letters (2005-11-03)
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, Joseph P Vacca
PMID16263281
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 beta-secretase inhibitor 7m which has an in vitro IC(50)=35 nM. The synthesis and biological activities of these compounds are described.