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Bioorg Med Chem Lett ; 16(3): 641-4, 2006 Feb.
Article in English | MEDLINE | ID: mdl-16263281

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.


Subject(s)
Amides/chemistry , Endopeptidases/metabolism , Protease Inhibitors/chemical synthesis , Amides/pharmacology , Amyloid Precursor Protein Secretases , Drug Design , Inhibitory Concentration 50 , Models, Molecular , Phthalic Acids/chemistry , Protease Inhibitors/pharmacology , Structure-Activity Relationship
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