Discovery of Adamantyl Heterocyclic Ketones as Potent 11β??Hydroxysteroid Dehydrogenase Type 1 Inhibitors

…, MP Thomas, F Pradaux??Caggiano, H Halem…

Index: Su, Xiangdong; Vicker, Nigel; Thomas, Mark P.; Pradaux-Caggiano, Fabienne; Halem, Heather; Culler, Michael D.; Potter, Barry V.L. ChemMedChem, 2011 , vol. 6, # 8 p. 1439 - 1451

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Citation Number: 9

Abstract

Abstract 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) plays a key role in converting intracellular cortisone to physiologically active cortisol, which is implicated in the development of several phenotypes of metabolic syndrome. Inhibition of 11β-HSD1 activity with selective inhibitors has beneficial effects on various conditions, including diabetes, dyslipidemia and obesity, and therefore constitutes a promising strategy to discover novel ...