Synthesis and Biological Evaluation of Sulfonamidooxazoles and Β-Keto Sulfones: Selective Inhibitors of 11Β-Hydroxysteroid Dehydrogenase Type I

The design, synthesis, and biological evaluation of arylsulfonamidooxazoles as 11β-HSD1 inhibitors and the serendipitous discovery of β-keto sulfones as potent 11β-HSD1 inhibitors are described here. These two classes of compounds are not active against 11β-HSD2 and therefore may have significant therapeutic potential for metabolic syndrome, type 2 diabetes and related metabolic dysfunctions.