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Bioorg Med Chem Lett. 2006 Feb;16(3):641-4. Epub 2005 Nov 2.

Conformationally biased P3 amide replacements of beta-secretase inhibitors.

Author information

1
Department 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.

PMID:
16263281
DOI:
10.1016/j.bmcl.2005.10.032
[Indexed for MEDLINE]

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