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, 20 (9), 2837-42

Piperazine Sulfonamide BACE1 Inhibitors: Design, Synthesis, and in Vivo Characterization

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Piperazine Sulfonamide BACE1 Inhibitors: Design, Synthesis, and in Vivo Characterization

Jared Cumming et al. Bioorg Med Chem Lett.

Abstract

With collaboration between chemistry, X-ray crystallography, and molecular modeling, we designed and synthesized a series of novel piperazine sulfonamide BACE1 inhibitors. Iterative exploration of the non-prime side and S2' sub-pocket of the enzyme culminated in identification of an analog that potently lowers peripheral Abeta(40) in transgenic mice with a single subcutaneous dose.

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