N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11β-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275

…, J Ermolieff, A Castro, NA Hosea, A LaPaglia…

Index: Siu, Michael; Johnson, Theodore O.; Wang, Yong; Nair, Sajiv K.; Taylor, Wendy D.; Cripps, Stephan J.; Matthews, Jean J.; Edwards, Martin P.; Pauly, Thomas A.; Ermolieff, Jacques; Castro, Arturo; Hosea, Natilie A.; LaPaglia, Amy; Fanjul, Andrea N.; Vogel, Jennifer E. Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 13 p. 3493 - 3497

Full Text: HTML

Citation Number: 37

Abstract

N-(Pyridin-2-yl) arylsulfonamides are identified as inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1), an enzyme that catalyzes the reduction of the glucocorticoid cortisone to cortisol. Dysregulation of glucocorticoids has been implicated in the pathogenesis of diabetes and the metabolic syndrome. In this Letter, we present the development of an initial lead to an efficient ligand with improved physiochemical ...