Abstract
This letter describes replacements for the P3 amide moiety present in previously reported tertiary carbinamine macrolactones. Although P-gp efflux issues associated with these amide-macrolactones were solved and full brain penetration was measured in one case, potency was compromised in the process.
MeSH terms
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Amines / pharmacokinetics*
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Amyloid Precursor Protein Secretases / antagonists & inhibitors*
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Aspartic Acid Endopeptidases / antagonists & inhibitors*
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Brain / metabolism*
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Crystallography, X-Ray
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Enzyme Inhibitors / pharmacokinetics*
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Models, Molecular
Substances
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Amines
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Enzyme Inhibitors
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Amyloid Precursor Protein Secretases
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Aspartic Acid Endopeptidases
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BACE1 protein, human