Piperidine amides as 11beta-hydroxysteroid dehydrogenase type 1 inhibitors.
A series of piperidine amide inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) were identified via modifications of the HTS hit compound 1. The synthesis, in vitro biological evaluation, and structure-activity relationship of these compounds are presented.
Flyrén
Katarina
K
Biovitrum AB, SE-112 76 Stockholm, Sweden. katarina.flyren@biovitrum.com
Bergquist
Lars O
LO
Castro
Victor M
VM
Fotsch
Christopher
C
Johansson
Lars
L
St Jean
David J
DJ
Sutin
Lori
L
Williams
Meredith
M
D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1 / Q000037:antagonists & inhibitors*; D000577:Amides / Q000737:chemistry / Q000494:pharmacology*; D001665:Binding Sites; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D006801:Humans; D007124:Immunoenzyme Techniques; D008956:Models, Chemical; D010880:Piperidines / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000577:Amides; D004791:Enzyme Inhibitors; D010880:Piperidines; C032727:piperidine; D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1