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Bioorg Med Chem. 2008 Nov 1;16(21):9471-86. doi: 10.1016/j.bmc.2008.09.041. Epub 2008 Sep 19.

Design, synthesis and SAR of potent statine-based BACE-1 inhibitors: exploration of P1 phenoxy and benzyloxy residues.

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1
Department of Chemistry, Linköping University, S-58183 Linköping, Sweden.

Abstract

Several BACE-1 inhibitors with low nanomolar level activities, encompassing a statine-based core structure with phenyloxymethyl- and benzyloxymethyl residues in the P1 position, are presented. The novel P1 modification introduced to allow the facile exploration of the S1 binding pocket of BACE-1, delivered highly promising inhibitors.

PMID:
18842420
DOI:
10.1016/j.bmc.2008.09.041
[Indexed for MEDLINE]
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