Abstract
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.
MeSH terms
-
11-beta-Hydroxysteroid Dehydrogenase Type 1 / antagonists & inhibitors*
-
Amides / chemistry
-
Amides / pharmacology*
-
Binding Sites
-
Enzyme Inhibitors / chemical synthesis
-
Enzyme Inhibitors / pharmacology*
-
Humans
-
Immunoenzyme Techniques
-
Models, Chemical
-
Piperidines / chemistry
-
Piperidines / pharmacology*
-
Structure-Activity Relationship
Substances
-
Amides
-
Enzyme Inhibitors
-
Piperidines
-
piperidine
-
11-beta-Hydroxysteroid Dehydrogenase Type 1