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  • Title: Design and synthesis of statine-containing BACE inhibitors.
    Author: Hu J, Cwi CL, Smiley DL, Timm D, Erickson JA, McGee JE, Yang HC, Mendel D, May PC, Shapiro M, McCarthy JR.
    Journal: Bioorg Med Chem Lett; 2003 Dec 15; 13(24):4335-9. PubMed ID: 14643321.
    Abstract:
    Utilizing structure-based techniques and solid-phase synthesis, statine-based tetrapeptide BACE inhibitors were designed and synthesized using a heptapeptide BACE transition-state mimetic, 1, as the starting point. Structure-activity relationship studies at the P(3), P(2), and P(2)' positions as well as the N-terminal capping group on scaffold 5 led to the discovery of potent inhibitors 27, 32, and 34 (IC(50) <100 nM). In addition, computational analysis and the X-ray structure of BACE-inhibitor 38 are discussed.
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