title: Adamantane sulfone and sulfonamide 11-beta-HSD1 Inhibitors.
abstract: Potent and selective adamantane sulfone and sulfonamide inhibitors of 11-beta-HSD-1 have been discovered. Selected compounds from these series have robust pharmacokinetic profiles and strongly inhibit liver, fat, and brain HSD1 for extended periods after oral dosing.
authors.affiliation: Abbott, Dept. 47F, Bldg. AP-10, Rm. 301, 100 Abbott Park Road, Abbott Park, IL 60064-6098, USA.
authors.forename: Bryan
authors.initials: B
authors.lastname: Sorensen
authors.forename: Martin
authors.initials: M
authors.lastname: Winn
authors.forename: Jeff
authors.initials: J
authors.lastname: Rohde
authors.forename: Qi
authors.initials: Q
authors.lastname: Shuai
authors.forename: Jiahong
authors.initials: J
authors.lastname: Wang
authors.forename: Steven
authors.initials: S
authors.lastname: Fung
authors.forename: Katina
authors.initials: K
authors.lastname: Monzon
authors.forename: William
authors.initials: W
authors.lastname: Chiou
authors.forename: DeAnne
authors.initials: D
authors.lastname: Stolarik
authors.forename: Hovis
authors.initials: H
authors.lastname: Imade
authors.forename: Liping
authors.initials: L
authors.lastname: Pan
authors.forename: Xiaoqing
authors.initials: X
authors.lastname: Deng
authors.forename: Linda
authors.initials: L
authors.lastname: Chovan
authors.forename: Kenton
authors.initials: K
authors.lastname: Longenecker
authors.forename: Russell
authors.initials: R
authors.lastname: Judge
authors.forename: Wenying
authors.initials: W
authors.lastname: Qin
authors.forename: Michael
authors.initials: M
authors.lastname: Brune
authors.forename: Heidi
authors.initials: H
authors.lastname: Camp
authors.forename: Ernst U
authors.initials: EU
authors.lastname: Frevert
authors.forename: Peer
authors.initials: P
authors.lastname: Jacobson
authors.forename: J T
authors.initials: JT
authors.lastname: Link
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* / Q000138:chemical synthesis* / Q000494:pharmacology*; D000273:Adipose Tissue / Q000201:enzymology; D000818:Animals; D001921:Brain / Q000201:enzymology; D018360:Crystallography, X-Ray; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D006801:Humans; D007202:Indicators and Reagents; D008099:Liver / Q000201:enzymology; D051379:Mice; D008958:Models, Molecular; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D007202:Indicators and Reagents; D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1; D043209:11-beta-Hydroxysteroid Dehydrogenase Type 2; D000218:Adamantane