Abstract
The design and synthesis of a novel series of potent BACE1 hydroxyethylamine inhibitors. These inhibitors feature hydrogen bonding substituents at the C-5 position of the isophthalamide ring with improved selectivity over cathepsin D.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
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Amyloid Precursor Protein Secretases / antagonists & inhibitors*
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Animals
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Aspartic Acid Endopeptidases / antagonists & inhibitors*
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Cathepsin D / antagonists & inhibitors
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Drug Design
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / pharmacology*
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Ethylamines / chemical synthesis
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Ethylamines / pharmacology*
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Humans
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Hydrogen Bonding
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Ifosfamide / analogs & derivatives
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Ifosfamide / chemical synthesis
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Ifosfamide / pharmacology*
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Mice
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Mice, Knockout
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Models, Chemical
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Structure-Activity Relationship
Substances
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Enzyme Inhibitors
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Ethylamines
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Amyloid Precursor Protein Secretases
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Aspartic Acid Endopeptidases
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BACE1 protein, human
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Bace1 protein, mouse
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Cathepsin D
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Ifosfamide