11β-HSD1 inhibition is a potential therapeutic target for a broad range of disorders including obesity that could be improved by decreased intracellular cortisol levels determined with an HTRF assay
A new series of cyclic sulfonamide derivatives was synthesized and evaluated for their ability to inhibit 11beta-HSD1. Cyclic sulfonamides with phenylacetyl substituents at the 2-position showed nanomolar inhibitory activities. Among them, compound 4e exhibited a good in vitro inhibitory activity and selectivity toward human 11beta-HSD2.
Bioorg Med Chem Lett. 2010;20(3):1065-9.