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Bioorg Med Chem Lett. 2007 Oct 1;17(19):5353-6. Epub 2007 Aug 11.

Thiophene substituted acylguanidines as BACE1 inhibitors.

Author information

1
Chemical and Screening Sciences, Wyeth Research, CN8000, Princeton, NJ 08543-8000, USA. fobarew@wyeth.com

Abstract

A series of thiophene-substituted acylguanidines were designed from a pyrrole substituted acylguanidine HTS lead. This template allowed a greater flexibility, through differential Suzuki couplings, to explore the binding site of BACE1 and to enhance the inhibitory potencies. This exploration provided a 25-fold enhancement in potency to yield compound 10a, which was 150 nM in a BACE1 FRET assay.

PMID:
17761418
DOI:
10.1016/j.bmcl.2007.08.010
[Indexed for MEDLINE]

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