title: Modulation of 11beta-hydroxysteroid dehydrogenase type 1 activity by 1,5-substituted 1H-tetrazoles.
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.
authors.affiliation: Endocrinology Unit, Centre for Cardiovascular Science, The Queen's Medical Research Institute, University of Edinburgh, 47 Little France Crescent, Edinburgh EH16 4TJ, UK. scott.webster@ed.ac.uk
authors.forename: Scott P
authors.initials: SP
authors.lastname: Webster
authors.forename: Margaret
authors.initials: M
authors.lastname: Binnie
authors.forename: Kirsty M M
authors.initials: KM
authors.lastname: McConnell
authors.forename: Karen
authors.initials: K
authors.lastname: Sooy
authors.forename: Peter
authors.initials: P
authors.lastname: Ward
authors.forename: Michael F
authors.initials: MF
authors.lastname: Greaney
authors.forename: Andy
authors.initials: A
authors.lastname: Vinter
authors.forename: T David
authors.initials: TD
authors.lastname: Pallin
authors.forename: Hazel J
authors.initials: HJ
authors.lastname: Dyke
authors.forename: Matthew I A
authors.initials: MI
authors.lastname: Gill
authors.forename: Ines
authors.initials: I
authors.lastname: Warner
authors.forename: Jonathan R
authors.initials: JR
authors.lastname: Seckl
authors.forename: Brian R
authors.initials: BR
authors.lastname: Walker
mesh_terms: D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1 / Q000037:antagonists & inhibitors*; D000818:Animals; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D006801:Humans; D051379:Mice; D008958:Models, Molecular; D013777:Tetrazoles / Q000494:pharmacology*
chemical_list: D004791:Enzyme Inhibitors; D013777:Tetrazoles; D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1
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