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

Abstract

WO2008052638 describes the identification and synthesis of diazepane– acetamide derivatives as a novel class of selective small molecule inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-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 11β-HSD1 as well as interference with alternative functions of this enzyme are needed to explore the therapeutic potential of these chemicals.

Keywords::

• 11β-hydroxysteroid dehydrogenase
• diabetes
• glucocorticoid
• inhibitor
• metabolic syndrome
• obesity

Acknowledgments

AO is supported by the Swiss National Science Foundation, grant A0310000-112279 and has a chair in Molecular and Systems Toxicology by the Novartis Research Foundation.

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