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Conformationally biased P3 amide replacements of beta-secretase inhibitors
Shawn J Stachel1, Craig A Coburn, Thomas G Steele
1Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. shawn_stachel@merck.com
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.
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