17649-96-6Relevant articles and documents
Modulation of 11β-hydroxysteroid dehydrogenase type 1 activity by 1,5-substituted 1H-tetrazoles
Webster, Scott P.,Binnie, Margaret,McConnell, Kirsty M.M.,Sooy, Karen,Ward, Peter,Greaney, Michael F.,Vinter, Andy,Pallin, T. David,Dyke, Hazel J.,Gill, Matthew I.A.,Warner, Ines,Seckl, Jonathan R.,Walker, Brian R.
scheme or table, p. 3265 - 3271 (2010/09/14)
Inhibitors of 11β-hydroxysteroid dehydrogenase (11β-HSD1) show promise as drugs to treat metabolic disease and CNS disorders such as cognitive impairment. A series of 1,5-substituted 1H-tetrazole 11β-HSD1 inhibitors has been discovered and chemically modified. Compounds are selective for 11β-HSD1 over 11β-HSD2 and possess good cellular potency in human and murine 11β-HSD1 assays. A range of in vitro stabilities are observed in human liver microsome assays.