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ID: ALA1759916

Journal: Bioorg Med Chem Lett

Title: Bicyclo[2.2.2]octyltriazole inhibitors of 11β-hydoxysteroid dehydrogenase type 1. Pharmacological agents for the treatment of metabolic syndrome.

Authors: Maletic M, Leeman A, Szymonifka M, Mundt SS, Zokian HJ, Shah K, Dragovic J, Lyons K, Thieringer R, Vosatka AH, Balkovec J, Waddell ST.

Abstract: Following the discovery of a metabolic 'soft-spot' on a bicyclo[2.2.2]octyltriazole lead, an extensive effort was undertaken to block the oxidative metabolism and improve PK of this potent HSD1 lead. In this communication, SAR survey focusing on various alkyl chain replacements will be detailed. This effort culminated in the discovery of a potent ethyl sulfone inhibitor with an improved PK profile across species and improved physical properties.

CiteXplore: 21421311

DOI: 10.1016/j.bmcl.2011.01.018