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Design, synthesis and SAR of potent statine-based BACE-1 inhibitors: exploration of P1 phenoxy and benzyloxy residues
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2008 (English)In: Bioorganic & Medicinal Chemistry, ISSN 0968-0896, E-ISSN 1464-3391, Vol. 16, no 21, 9471-86 p.Article in journal (Refereed) Published
Abstract [en]

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.

Place, publisher, year, edition, pages
2008. Vol. 16, no 21, 9471-86 p.
Keyword [en]
Alzheimer’s disease, BACE-1 inhibitors, P1 modifications, Peptidomimetics
National Category
Medical and Health Sciences
Identifiers
URN: urn:nbn:se:uu:diva-102900DOI: 10.1016/j.bmc.2008.09.041ISI: 000260134400010PubMedID: 18842420OAI: oai:DiVA.org:uu-102900DiVA: diva2:216965
Available from: 2009-05-12 Created: 2009-05-12 Last updated: 2017-12-13Bibliographically approved

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