Abstract
The thiazole-diamide series (1) has been identified as highly potent gamma-secretase inhibitors. Several representative compounds showed IC(50) values of <0.3 nM. The synthesis and SAR, as well as a radiolabeled synthesis of [(3)H]-2a, are described.
MeSH terms
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Alkylation
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Amination
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Amyloid Precursor Protein Secretases / antagonists & inhibitors*
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Amyloid Precursor Protein Secretases / metabolism
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Cell-Free System
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Diamide / chemical synthesis
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Diamide / chemistry*
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Diamide / pharmacology*
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Magnetic Resonance Spectroscopy
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Molecular Structure
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Structure-Activity Relationship
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Thiazoles / chemistry*
Substances
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Thiazoles
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Diamide
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Amyloid Precursor Protein Secretases