Modulation of 11beta-hydroxysteroid dehydrogenase type 1 activity by 1,5-substituted 1H-tetrazoles.
Basic Information
ID: ALA1155502
Journal: Bioorg Med Chem Lett
Title: Modulation of 11beta-hydroxysteroid dehydrogenase type 1 activity by 1,5-substituted 1H-tetrazoles.
Authors: Webster SP, Binnie M, McConnell KM, Sooy K, Ward P, Greaney MF, Vinter A, Pallin TD, Dyke HJ, Gill MI, Warner I, Seckl JR, Walker BR.
Abstract: Inhibitors of 11beta-hydroxysteroid dehydrogenase (11beta-HSD1) show promise as drugs to treat metabolic disease and CNS disorders such as cognitive impairment. A series of 1,5-substituted 1H-tetrazole 11beta-HSD1 inhibitors has been discovered and chemically modified. Compounds are selective for 11beta-HSD1 over 11beta-HSD2 and possess good cellular potency in human and murine 11beta-HSD1 assays. A range of in vitro stabilities are observed in human liver microsome assays.
CiteXplore: 20452767
DOI: 10.1016/j.bmcl.2010.04.055
Patent ID: ┄