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, 17 (19), 5353-6

Thiophene Substituted Acylguanidines as BACE1 Inhibitors

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Thiophene Substituted Acylguanidines as BACE1 Inhibitors

William F Fobare et al. Bioorg Med Chem Lett.

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.

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