Diazepane-acetamide derivatives as selective 11beta-hydroxysteroid dehydrogenase type 1 inhibitors.
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.
Odermatt
Alex
A
University of Basel, Division of Molecular and Systems Toxicology, Department of Pharmaceutical Sciences, Klingelbergstrasse 50, Basel, Switzerland. alex.odermatt@unibas.ch
D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D000081:Acetamides / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D001381:Azepines / Q000737:chemistry / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D024821:Metabolic Syndrome / Q000188:drug therapy* / Q000201:enzymology; D015394:Molecular Structure; D010330:Patents as Topic; D013329:Structure-Activity Relationship
D000081:Acetamides; D001381:Azepines; D004791:Enzyme Inhibitors; D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1