The discovery of azepane sulfonamides as potent 11β-HSD1 inhibitors

SF Neelamkavil, CD Boyle, S Chackalamannil…

Index: Neelamkavil, Santhosh F.; Boyle, Craig D.; Chackalamannil, Samuel; Greenlee, William J.; Zhang, Lili; Terracina, Giuseppe Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 16 p. 4563 - 4565

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Citation Number: 10

Abstract

Discovery of a series of azepine sulfonamides as potent inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) is described. SAR studies at the 4-position of the azepane ring have resulted in the discovery of a very potent compound 30 which has an 11β- HSD1 IC50 of 3.0 nM.