Adamantyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1

Bioorg Med Chem Lett. 2005 Oct 1;15(19):4359-62. doi: 10.1016/j.bmcl.2005.06.040.

Abstract

Adamantyl triazoles were identified as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1). They are active both in in vitro and in in vivo pharmacodynamic models. The synthesis and structure-activity relationships of these inhibitors are presented.

MeSH terms

  • 11-beta-Hydroxysteroid Dehydrogenase Type 1 / antagonists & inhibitors*
  • Adamantane / chemical synthesis
  • Adamantane / pharmacokinetics
  • Adamantane / pharmacology
  • Animals
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / pharmacokinetics
  • Enzyme Inhibitors / pharmacology
  • Humans
  • Inhibitory Concentration 50
  • Metabolic Syndrome / drug therapy
  • Mice
  • Pharmacokinetics
  • Structure-Activity Relationship
  • Triazoles / chemical synthesis*
  • Triazoles / pharmacokinetics
  • Triazoles / pharmacology

Substances

  • Enzyme Inhibitors
  • Triazoles
  • 11-beta-Hydroxysteroid Dehydrogenase Type 1
  • Adamantane