Design, synthesis and SAR of potent statine-based BACE-1 inhibitors: exploration of P1 phenoxy and benzyloxy residues.
2008 (English)In: Bioorganic & medicinal chemistry, ISSN 1464-3391, Vol. 16, no 21, 9471-9486 p.Article in journal (Refereed) Published
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, 9471-9486 p.
Alzheimer’s disease, BACE-1 inhibitors, P1 modifications, Peptidomimetics
National CategoryNatural Sciences
IdentifiersURN: urn:nbn:se:liu:diva-17848DOI: 10.1016/j.bmc.2008.09.041PubMedID: 18842420OAI: oai:DiVA.org:liu-17848DiVA: diva2:212502