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Design, synthesis, and structure-activity relationship studies of N-arylsulfonyl morpholines as γ-secretase inhibitors.

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.
AuthorsHongmei Li, Ruo Xu, David Cole, John W Clader, William J Greenlee, Amin A Nomeir, Lixin Song, Lili Zhang
JournalBioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 20 Issue 22 Pg. 6606-9 (Nov 15 2010) ISSN: 1464-3405 [Electronic] England
PMID20933414 (Publication Type: Journal Article)
CopyrightCopyright © 2010 Elsevier Ltd. All rights reserved.
Chemical References
  • Enzyme Inhibitors
  • Morpholines
  • Amyloid Precursor Protein Secretases
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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