Modulation of 11beta-hydroxysteroid dehydrogenase type 1 activity by 1,5-substituted 1H-tetrazoles

Scott P. Webster, Margaret Binnie, Kirsty M. M. McConnell, Karen Sooy, Peter Ward, Michael F. Greaney, Andy Vinter, T. David Pallin, Hazel J. Dyke, Matthew I. A. Gill, Ines Warner, Jonathan R. Seckl, Brian R. Walker

Research output: Contribution to journalArticlepeer-review

Abstract

Inhibitors of 11beta-hydroxysteroid dehydrogenase (11beta-HSD1) show promise as drugs to treat metabolic disease and CNS disorders such as cognitive impairment. A series of 1,5-substituted 1H-tetrazole 11beta-HSD1 inhibitors has been discovered and chemically modified. Compounds are selective for 11beta-HSD1 over 11beta-HSD2 and possess good cellular potency in human and murine 11beta-HSD1 assays. A range of in vitro stabilities are observed in human liver microsome assays.
Original languageEnglish
Pages (from-to)3265-3271
Number of pages7
JournalBioorganic & Medicinal Chemistry Letters
Volume20
Issue number11
DOIs
Publication statusPublished - 1 Jun 2010

Keywords

  • 11β-Hydroxysteroid dehydrogenase type 1
  • 11β-HSD1
  • Drug discovery
  • Metabolic syndrome

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