Discovery of cyclicsulfonamide derivatives as 11 beta-hydroxysteroid dehydrogenase 1 inhibitors

作者：Kim Se Hoan; Ramu Ravirala; Kwon Sung Wook; Lee Su Hee; Kim Chi Hyun; Kang Seung Kyu; Rhee Sang Dal; Bae Myung Ae; Ahn Sung Hoon; Ha Duck Chan; Cheon Hyae Gyeong; Kim Ki Young^*; Ahn Jin Hee

来源：Bioorganic & Medicinal Chemistry Letters, 2010, 20(3): 1065-1069.

DOI：10.1016/j.bmcl.2009.12.035

• 11 beta-Hydroxysteroid dehydrogenase 1
• Cyclic sulfonamide
• Diabetes
• Inhibitor

A new series of cyclic sulfonamide derivatives was synthesized and evaluated for their ability to inhibit 11 beta-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 11 beta-HSD2.

• 出版日期2010-2-1