title: Oxazolones as potent inhibitors of 11beta-hydroxysteroid dehydrogenase type 1.
abstract: 2,5,5-Trisubstituted oxazolones were identified as potent inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1). The synthesis, structure-activity relationship and metabolic stability of these compounds are presented.
authors.affiliation: Biovitrum AB, SE-112 76, Stockholm, Sweden. lori.sutin@biovitrum.com
authors.forename: Lori
authors.initials: L
authors.lastname: Sutin
authors.forename: Sören
authors.initials: S
authors.lastname: Andersson
authors.forename: Lars
authors.initials: L
authors.lastname: Bergquist
authors.forename: Victor M
authors.initials: VM
authors.lastname: Castro
authors.forename: Eva
authors.initials: E
authors.lastname: Danielsson
authors.forename: Stephen
authors.initials: S
authors.lastname: James
authors.forename: Martin
authors.initials: M
authors.lastname: Henriksson
authors.forename: Lars
authors.initials: L
authors.lastname: Johansson
authors.forename: Christina
authors.initials: C
authors.lastname: Kaiser
authors.forename: Katarina
authors.initials: K
authors.lastname: Flyrén
authors.forename: Meredith
authors.initials: M
authors.lastname: Williams
mesh_terms: D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1 / Q000037:antagonists & inhibitors*; D000818:Animals; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D003348:Cortisone / Q000737:chemistry; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D006854:Hydrocortisone / Q000737:chemistry; D008956:Models, Chemical; D010080:Oxazoles / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000737:chemistry
chemical_list: D004791:Enzyme Inhibitors; D010080:Oxazoles; D013844:Thiazoles; D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1; D003348:Cortisone; D006854:Hydrocortisone