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

Bioorg Med Chem Lett. 2008 May 1;18(9):2799-804. doi: 10.1016/j.bmcl.2008.04.010. Epub 2008 Apr 9.

Abstract

3-Aryl-5-phenyl-(1,2,4)-triazoles were identified as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1). They are active in both in vitro and an in vivo mouse pharmacodynamic (PD) model. The synthesis and structure activity relationships are presented.

MeSH terms

  • 11-beta-Hydroxysteroid Dehydrogenase Type 1 / antagonists & inhibitors*
  • Animals
  • Binding Sites
  • Disease Models, Animal
  • Enzyme Inhibitors* / chemical synthesis
  • Enzyme Inhibitors* / pharmacokinetics
  • Enzyme Inhibitors* / therapeutic use
  • Hydrocarbons, Aromatic* / chemical synthesis
  • Hydrocarbons, Aromatic* / pharmacology
  • Hydrocarbons, Aromatic* / therapeutic use
  • Hypoglycemic Agents* / chemical synthesis
  • Hypoglycemic Agents* / pharmacokinetics
  • Hypoglycemic Agents* / therapeutic use
  • Inhibitory Concentration 50
  • Metabolic Syndrome / drug therapy*
  • Mice
  • Models, Chemical
  • Structure-Activity Relationship
  • Triazoles* / chemical synthesis
  • Triazoles* / pharmacology
  • Triazoles* / therapeutic use

Substances

  • Enzyme Inhibitors
  • Hydrocarbons, Aromatic
  • Hypoglycemic Agents
  • Triazoles
  • 11-beta-Hydroxysteroid Dehydrogenase Type 1