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Bioorg Med Chem Lett. 2010 May 1;20(9):2837-42. doi: 10.1016/j.bmcl.2010.03.050. Epub 2010 Mar 12.

Piperazine sulfonamide BACE1 inhibitors: design, synthesis, and in vivo characterization.

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1
Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. jared.cumming@merck.com

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.

PMID:
20347593
DOI:
10.1016/j.bmcl.2010.03.050
[Indexed for MEDLINE]
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