Conformationally biased P3 amide replacements of beta-secretase inhibitors.
Stachel, S.J., Coburn, C.A., Steele, T.G., Crouthamel, M.-C., Pietrak, B.L., Lai, M.-T., Holloway, M.K., Munshi, S.K., Graham, S.L., Vacca, J.P.(2006) Bioorg Med Chem Lett 16: 641-644
- PubMed: 16263281 
- DOI: https://doi.org/10.1016/j.bmcl.2005.10.032
- Primary Citation of Related Structures:  
2B8L, 2B8V - PubMed 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.
Organizational Affiliation: 
Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. [email protected]