Abstract
The synthesis and gamma-secretase inhibition data for a series of nitrogen-appended N-alkylsulfonamides (11-47) are described. Inhibition of brain Abeta in transgenic mice was demonstrated by two of these compounds (23 and 44).
MeSH terms
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Alkylation
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Amines / chemical synthesis
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Amines / chemistry*
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Amines / pharmacology*
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Amyloid Precursor Protein Secretases / antagonists & inhibitors*
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Amyloid beta-Peptides / genetics
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Amyloid beta-Peptides / metabolism
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Animals
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Azoles / chemical synthesis
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Azoles / chemistry
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Azoles / pharmacology
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Brain / drug effects
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Brain / enzymology
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Brain / metabolism
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Hydrophobic and Hydrophilic Interactions
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Inhibitory Concentration 50
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Mice
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Mice, Transgenic
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Peptide Fragments / metabolism
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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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Structure-Activity Relationship
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Sulfonamides / chemical synthesis
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Sulfonamides / chemistry*
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Sulfonamides / pharmacology*
Substances
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Amines
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Amyloid beta-Peptides
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Azoles
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Peptide Fragments
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Protease Inhibitors
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Sulfonamides
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amyloid beta-protein (1-40)
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Amyloid Precursor Protein Secretases