Discovery of adamantyl heterocyclic ketones as potent 11 beta-hydroxysteroid dehydrogenase type 1 inhibitors
Su, X., Vicker, N., Thomas, M. P., Pradaux-Caggiano, F., Halem, H., Culler, M. D. and Potter, B. V. L., 2011. Discovery of adamantyl heterocyclic ketones as potent 11 beta-hydroxysteroid dehydrogenase type 1 inhibitors. ChemMedChem, 6 (8), pp. 1439-1451.
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11 beta-Hydroxysteroid dehydrogenase type 1 (11 beta-HSD1) plays a key role in converting intracellular cortisone to physiologically active cortisol, which is implicated in the development of several phenotypes of metabolic syndrome. Inhibition of 11 beta-HSD1 activity with selective inhibitors has beneficial effects on various conditions, including diabetes, dyslipidemia and obesity, and therefore constitutes a promising strategy to discover novel therapies for metabolic and cardiovascular diseases. A series of novel adamantyl heterocyclic ketones provides potent and selective inhibitors of human 11 beta-HSD1. Lead compounds display low nanomolar inhibition against human and mouse 11 beta-HSD1 and are selective with no activity against 11 beta-HSD2 and 17 beta-HSD1. Selected potent 11 beta-HSD1 inhibitors show moderate metabolic stability upon incubation with human liver microsomes and weak inhibition of human CYP450 enzymes.
|Creators||Su, X., Vicker, N., Thomas, M. P., Pradaux-Caggiano, F., Halem, H., Culler, M. D. and Potter, B. V. L.|
|Departments||Faculty of Science > Pharmacy & Pharmacology|
Faculty of Science > Chemistry
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