title: Bis-aryl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1.
abstract: 3-Aryl-5-phenyl-(1,2,4)-triazoles were identified as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1). They are active in both in vitro and an in vivo mouse pharmacodynamic (PD) model. The synthesis and structure activity relationships are presented.
authors.affiliation: Department of Medicinal Chemistry, Merck & Co., Inc., PO Box 2000, Rahway, NJ 07065, USA. susan_aster@merck.com
authors.forename: Susan D
authors.initials: SD
authors.lastname: Aster
authors.forename: Donald W
authors.initials: DW
authors.lastname: Graham
authors.forename: Divya
authors.initials: D
authors.lastname: Kharbanda
authors.forename: Gool
authors.initials: G
authors.lastname: Patel
authors.forename: Mitree
authors.initials: M
authors.lastname: Ponpipom
authors.forename: Gina M
authors.initials: GM
authors.lastname: Santorelli
authors.forename: Michael J
authors.initials: MJ
authors.lastname: Szymonifka
authors.forename: Steven S
authors.initials: SS
authors.lastname: Mundt
authors.forename: Kashmira
authors.initials: K
authors.lastname: Shah
authors.forename: Marty S
authors.initials: MS
authors.lastname: Springer
authors.forename: Rolf
authors.initials: R
authors.lastname: Thieringer
authors.forename: Anne
authors.initials: A
authors.lastname: Hermanowski-Vosatka
authors.forename: Samuel D
authors.initials: SD
authors.lastname: Wright
authors.forename: Jianying
authors.initials: J
authors.lastname: Xiao
authors.forename: Hratch
authors.initials: H
authors.lastname: Zokian
authors.forename: James M
authors.initials: JM
authors.lastname: Balkovec
mesh_terms: D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1 / Q000037:antagonists & inhibitors*; D000818:Animals; D001665:Binding Sites; D004195:Disease Models, Animal; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000627:therapeutic use; D006841:Hydrocarbons, Aromatic / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use; D007004:Hypoglycemic Agents / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000627:therapeutic use; D020128:Inhibitory Concentration 50; D024821:Metabolic Syndrome / Q000188:drug therapy*; D051379:Mice; D008956:Models, Chemical; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use
chemical_list: D004791:Enzyme Inhibitors; D006841:Hydrocarbons, Aromatic; D007004:Hypoglycemic Agents; D014230:Triazoles; D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1