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ID: ALA1137439

Journal: Bioorg Med Chem Lett

Title: Thiophene substituted acylguanidines as BACE1 inhibitors.

Authors: Fobare WF, Solvibile WR, Robichaud AJ, Malamas MS, Manas E, Turner J, Hu Y, Wagner E, Chopra R, Cowling R, Jin G, Bard J.

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.

CiteXplore: 17761418

DOI: 10.1016/j.bmcl.2007.08.010