title: Adamantyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1.
abstract: Adamantyl triazoles were identified as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1). They are active both in in vitro and in in vivo pharmacodynamic models. The synthesis and structure-activity relationships of these inhibitors are presented.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. steven_olson@merck.com
authors.forename: Steven
authors.initials: S
authors.lastname: Olson
authors.forename: Susan D
authors.initials: SD
authors.lastname: Aster
authors.forename: Kai
authors.initials: K
authors.lastname: Brown
authors.forename: Linda
authors.initials: L
authors.lastname: Carbin
authors.forename: Donald W
authors.initials: DW
authors.lastname: Graham
authors.forename: Anne
authors.initials: A
authors.lastname: Hermanowski-Vosatka
authors.forename: Cheryl B
authors.initials: CB
authors.lastname: LeGrand
authors.forename: Steven S
authors.initials: SS
authors.lastname: Mundt
authors.forename: Michael A
authors.initials: MA
authors.lastname: Robbins
authors.forename: James M
authors.initials: JM
authors.lastname: Schaeffer
authors.forename: Llnon H
authors.initials: LH
authors.lastname: Slossberg
authors.forename: Michael J
authors.initials: MJ
authors.lastname: Szymonifka
authors.forename: Rolf
authors.initials: R
authors.lastname: Thieringer
authors.forename: Samuel D
authors.initials: SD
authors.lastname: Wright
authors.forename: James M
authors.initials: JM
authors.lastname: Balkovec
mesh_terms: D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1 / Q000037:antagonists & inhibitors*; D000218:Adamantane / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology; D000818:Animals; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D024821:Metabolic Syndrome / Q000188:drug therapy; D051379:Mice; D010599:Pharmacokinetics; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology
chemical_list: D004791:Enzyme Inhibitors; D014230:Triazoles; D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1; D000218:Adamantane