Diazepane-acetamide derivatives as selective 11beta-hydroxysteroid dehydrogenase type 1 inhibitors

Expert Opin Ther Pat. 2009 Oct;19(10):1477-83. doi: 10.1517/13543770902911490.

Abstract

WO2008052638 describes the identification and synthesis of diazepane- acetamide derivatives as a novel class of selective small molecule inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) for the treatment of metabolic syndrome. The generic structure of the disclosed diazepane-acetamide derivatives offers considerable possibilities for modifications that allow optimizing compound properties. Further studies to assess target selectivity, species-specificity, modulation of tissue-specific functions of 11beta-HSD1 as well as interference with alternative functions of this enzyme are needed to explore the therapeutic potential of these chemicals.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 11-beta-Hydroxysteroid Dehydrogenase Type 1 / antagonists & inhibitors*
  • 11-beta-Hydroxysteroid Dehydrogenase Type 1 / metabolism
  • Acetamides / chemistry
  • Acetamides / pharmacology*
  • Animals
  • Azepines / chemistry
  • Azepines / pharmacology*
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • Humans
  • Metabolic Syndrome / drug therapy*
  • Metabolic Syndrome / enzymology
  • Molecular Structure
  • Patents as Topic
  • Structure-Activity Relationship

Substances

  • Acetamides
  • Azepines
  • Enzyme Inhibitors
  • 11-beta-Hydroxysteroid Dehydrogenase Type 1