Thiophene substituted acylguanidines as BACE1 inhibitors
Copyright policy )Thiophene substituted acylguanidines as BACE1 inhibitors
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.
- College of New Jersey United States
Models, Molecular, Thiophenes, Crystallography, X-Ray, Guanidines, Structure-Activity Relationship, Drug Design, Aspartic Acid Endopeptidases, Indicators and Reagents, Pyrroles, Amyloid Precursor Protein Secretases, Enzyme Inhibitors
Models, Molecular, Thiophenes, Crystallography, X-Ray, Guanidines, Structure-Activity Relationship, Drug Design, Aspartic Acid Endopeptidases, Indicators and Reagents, Pyrroles, Amyloid Precursor Protein Secretases, Enzyme Inhibitors
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