Discovery and biological evaluation of adamantyl amide 11beta-HSD1 inhibitors

Scott P Webster, Peter Ward, Margaret Binnie, Eilidh Craigie, Kirsty M M McConnell, Karen Sooy, Andy Vinter, Jonathan R Seckl, Brian R Walker

Research output: Contribution to journalArticlepeer-review

Abstract / Description of output

A series of adamantyl amide 11beta-HSD1 inhibitors has been discovered and chemically modified. Selected compounds are selective for 11beta-HSD1 over 11beta-HSD2 and possess excellent cellular potency in human and murine 11beta-HSD1 assays. Good pharmacodynamic characteristics are observed in ex vivo assays.
Original languageEnglish
Pages (from-to)2838-2843
Number of pages6
JournalBioorganic & Medicinal Chemistry Letters
Volume17
Issue number10
DOIs
Publication statusPublished - 15 May 2007

Keywords / Materials (for Non-textual outputs)

  • Metabolic syndrome
  • 11β-HSD1
  • 11β-HSD2
  • Inhibitor
  • Adamantane
  • Amide
  • Diabetes
  • 11β-Hydroxysteroid dehydrogenase
  • Enzyme inhibition
  • Hsd1

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