| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1365863 | Bioorganic & Medicinal Chemistry Letters | 2007 | 4 Pages |
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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Related Topics
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Chemistry
Organic Chemistry
Authors
William F. Fobare, William R. Solvibile, Albert J. Robichaud, Michael S. Malamas, Eric Manas, Jim Turner, Yun Hu, Erik Wagner, Rajiv Chopra, Rebecca Cowling, Guixan Jin, Jonathan Bard,