Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 13, Pages 3493-3497Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.05.011
Keywords
11-beta-Hydroxysteroid dehydrogenase; PF-915275; Diabetes; Lipophilic efficiency
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N-(Pyridin-2-yl) arylsulfonamides are identified as inhibitors of 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta HSD1), 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 properties using a deletion strategy. This strategy allowed for further optimization of potency leading to the discovery of the clinical candidate PF-915275. (C) 2009 Elsevier Ltd. All rights reserved.
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