Title of article
Thiophene substituted acylguanidines as BACE1 inhibitors
Author/Authors
William F. Fobare، نويسنده , , William R. Solvibile Jr.، نويسنده , , Albert J. Robichaud، نويسنده , , Michael S. Malamas، نويسنده , , Eric Manas، نويسنده , , Jim Turner، نويسنده , , Yun Hu، نويسنده , , Erik Wagner، نويسنده , , Rajiv Chopra، نويسنده , , Rebecca Cowling، نويسنده , , Guixan Jin، نويسنده , , Jonathan Bard، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
4
From page
5353
To page
5356
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.
Keywords
Beta-secretase , BACE1 , Aspartyl protease , Acylguanidine
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798612
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