title: Discovery and biological evaluation of adamantyl amide 11beta-HSD1 inhibitors.
abstract: A series of adamantyl amide 11beta-HSD1 inhibitors has been discovered and chemically modified. Selected compounds are selective for 11beta-HSD1 over 11beta-HSD2 and possess excellent cellular potency in human and murine 11beta-HSD1 assays. Good pharmacodynamic characteristics are observed in ex vivo 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: Peter
authors.initials: P
authors.lastname: Ward
authors.forename: Margaret
authors.initials: M
authors.lastname: Binnie
authors.forename: Eilidh
authors.initials: E
authors.lastname: Craigie
authors.forename: Kirsty M M
authors.initials: KM
authors.lastname: McConnell
authors.forename: Karen
authors.initials: K
authors.lastname: Sooy
authors.forename: Andy
authors.initials: A
authors.lastname: Vinter
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*; D043209:11-beta-Hydroxysteroid Dehydrogenase Type 2 / Q000037:antagonists & inhibitors; D000218:Adamantane / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology*; D000577:Amides / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D051379:Mice; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; D004791:Enzyme Inhibitors; D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1; D043209:11-beta-Hydroxysteroid Dehydrogenase Type 2; D000218:Adamantane