Abstract |
Design and synthesis of cis-2,6-disubstituted N-arylsulfonyl morpholines as novel γ- secretase inhibitors for the potential treatment of Alzheimer's disease (AD) is reported. Several different small alkyl groups are installed on the left-hand side to lower the CYP3A4 liability while maintaining excellent in vitro potency.
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Authors | Hongmei Li, Ruo Xu, David Cole, John W Clader, William J Greenlee, Amin A Nomeir, Lixin Song, Lili Zhang |
Journal | Bioorganic & medicinal chemistry letters
(Bioorg Med Chem Lett)
Vol. 20
Issue 22
Pg. 6606-9
(Nov 15 2010)
ISSN: 1464-3405 [Electronic] England |
PMID | 20933414
(Publication Type: Journal Article)
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Copyright | Copyright © 2010 Elsevier Ltd. All rights reserved. |
Chemical References |
- Enzyme Inhibitors
- Morpholines
- Amyloid Precursor Protein Secretases
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Topics |
- Amyloid Precursor Protein Secretases
(antagonists & inhibitors)
- Drug Design
- Enzyme Inhibitors
(chemical synthesis, chemistry, pharmacology)
- Morpholines
(chemical synthesis, chemistry, pharmacology)
- Structure-Activity Relationship
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