719274-28-9Relevant academic research and scientific papers
Bicyclo[2.2.2]octyltriazole inhibitors of 11β-hydoxysteroid dehydrogenase type 1. Pharmacological agents for the treatment of metabolic syndrome
Maletic, Milana,Leeman, Aaron,Szymonifka, Michael,Mundt, Steven S.,Zokian, Hratch J.,Shah, Kashmira,Dragovic, Jasminka,Lyons, Kathy,Thieringer, Rolf,Vosatka, Anne H.,Balkovec, James,Waddell, Sherman T.
, p. 2568 - 2572 (2011/05/15)
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.
Triazole derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase-1
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Page 52, (2008/06/13)
Triazole derivatives of structural formula I are selective inhibitors of the 11β-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resista
