Discovery of cyclicsulfonamide derivatives as 11beta-hydroxysteroid dehydrogenase 1 inhibitors.
Bioorganic & medicinal chemistry letters 2009 Dec 11; In press
Kim S SH, Ramu R, Kwon S SW, Lee S SH, Kim C CH, Kang S SK, Rhee S SD, Bae M MA, Ahn S SH, Ha D DC, Cheon H HG, Kim K KY, Ahn J JH
Department of Chemistry, Korea University, Seoul 121-742, Republic of Korea.
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.