Abstract
The 3,4-fused sulfamides, sulfonamides and sulfone have been identified as highly potent gamma-secretase inhibitors. Evaluation of the SAR of substitution within these series has allowed the identification of a range of compounds which significantly reduce brain A beta in transgenic mouse models and thus have potential as possible treatments for Alzheimer's disease.
MeSH terms
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Amyloid Precursor Protein Secretases
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Animals
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Aspartic Acid Endopeptidases
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Crystallography, X-Ray
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Cyclization
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Endopeptidases / metabolism*
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Models, Molecular
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Molecular Structure
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Protease Inhibitors / chemical synthesis*
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Protease Inhibitors / chemistry
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Protease Inhibitors / pharmacology*
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Rats
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Structure-Activity Relationship
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Sulfones / chemical synthesis
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Sulfones / chemistry*
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Sulfones / pharmacology*
Substances
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Protease Inhibitors
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Sulfones
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Amyloid Precursor Protein Secretases
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Endopeptidases
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Aspartic Acid Endopeptidases
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Bace1 protein, mouse