4.5 Article

Conformationally biased P3 amide replacements of β-secretase inhibitors

期刊

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 16, 期 3, 页码 641-644

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PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2005.10.032

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beta-secretase; P3; amide replacement

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yWe 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 IC50 = 35 nM. The synthesis and biological activities of these compounds are described. (c) 2005 Elsevier Ltd. All rights reserved.

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