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

Research output: Contribution to journalArticle

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


Inhibitors of 11β-hydroxysteroid dehydrogenase (11β-HSD1) show promise as drugs to treat metabolic disease and CNS disorders such as cognitive impairment. A series of 1,5-substituted 1H-tetrazole 11β-HSD1 inhibitors has been discovered and chemically modified. Compounds are selective for 11β-HSD1 over 11β-HSD2 and possess good cellular potency in human and murine 11β-HSD1 assays. A range of in vitro stabilities are observed in human liver microsome assays. © 2010 Elsevier Ltd. All rights reserved.

Bibliographical metadata

Original languageEnglish
Pages (from-to)3265-3271
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Issue number11
StatePublished - 1 Jun 2010