Conformationally biased P3 amide replacements of β-secretase inhibitors

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 β-secretase inhibitor 7m which has an in vitro IC50 = 35 nM. The synthesis and biological activities of these compounds are described.

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