title: Discovery of potent and selective inhibitors of 11beta-HSD1 for the treatment of metabolic syndrome.
abstract: High throughput screening efforts have identified a novel class of dichloroaniline amide 11beta-HSD1 inhibitors. SAR studies initiated from dichloroaniline 4 focused on retaining the potency and selectivity profile of the lead.
authors.affiliation: Metabolic Disease Research, GPRD, Abbott Laboratories, 100 Abbott Park Rd., Abbott Park, IL 60064, USA. Steven.Richards@abbott.com
authors.forename: Steven
authors.initials: S
authors.lastname: Richards
authors.forename: Bryan
authors.initials: B
authors.lastname: Sorensen
authors.forename: Hwan-Soo
authors.initials: HS
authors.lastname: Jae
authors.forename: Marty
authors.initials: M
authors.lastname: Winn
authors.forename: Yixian
authors.initials: Y
authors.lastname: Chen
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: Ernst U
authors.initials: EU
authors.lastname: Frevert
authors.forename: Peer
authors.initials: P
authors.lastname: Jacobson
authors.forename: Hing
authors.initials: H
authors.lastname: Sham
authors.forename: J T
authors.initials: JT
authors.lastname: Link
mesh_terms: D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1 / Q000037:antagonists & inhibitors*; D002229:Carbenoxolone / Q000737:chemistry / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000627:therapeutic use; D006801:Humans; D024821:Metabolic Syndrome / Q000188:drug therapy*; D008968:Molecular Conformation; D010879:Piperazines / Q000737:chemistry / Q000494:pharmacology; D013449:Sulfonamides / Q000737:chemistry / Q000494:pharmacology; D013844:Thiazoles / Q000737:chemistry / Q000494:pharmacology; D000096926:Benzenesulfonamides
chemical_list: D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1; D002229:Carbenoxolone; D004791:Enzyme Inhibitors; D010879:Piperazines; D013449:Sulfonamides; D013844:Thiazoles; C474501:3-chloro-2-methyl-N-(4-(2-(4-methyl-1-piperazinyl)-2-oxoethyl)-1,3-thiazol-2-yl)benzenesulfonamide; D000096926:Benzenesulfonamides