Synthesis of new glycyrrhetinic acid derived ring A azepanone, 29-urea and 29-hydroxamic acid derivatives as selective 11β-hydroxysteroid dehydrogenase 2 inhibitors

Starting from the natural compound glycyrrhetinic acid a set of 11β-HSD2 selective inhibitors was prepared. The most potent and most selective compound 28 is active against human 11β-HSD2 in the low nanomolar range with a more than 3600-fold selectivity over human 11β-HSD1.