Abstract
11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) is an enzyme involved in glucocorticoid regulation through catalysis of the conversion of inactive cortisone into its active form (cortisol). Chronically elevated local glucocorticoid level as a result of increased 11β-HSD1 activity is associated with metabolic syndrome, obesity, insulin resistance, type 2 diabetes mellitus, and cardiovascular complications. Inhibition of 11β-HSD1 has been proposed as a strategy to suppress glucocorticoid action in tissue-specific manner. In this article, we review a large variety of 11β-HSD1 inhibitors from various series of nitrogen-containing heterocycles, which are now under different stages of investigation as potential pharmacological agents for the treatment of metabolic syndrome, type 2 diabetes, and obesity.
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