Oxazolones as potent inhibitors of 11beta-hydroxysteroid dehydrogenase type 1.
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.
Sutin
Lori
L
Biovitrum AB, SE-112 76, Stockholm, Sweden. lori.sutin@biovitrum.com
Andersson
Sören
S
Bergquist
Lars
L
Castro
Victor M
VM
Danielsson
Eva
E
James
Stephen
S
Henriksson
Martin
M
Johansson
Lars
L
Kaiser
Christina
C
Flyrén
Katarina
K
Williams
Meredith
M
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
D004791:Enzyme Inhibitors; D010080:Oxazoles; D013844:Thiazoles; D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1; D003348:Cortisone; D006854:Hydrocortisone