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- W2035128931 abstract "Abstract 11β‐Hydroxysteroid dehydrogenase type 1 (11β‐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 11β‐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 11β‐HSD1. Lead compounds display low nanomolar inhibition against human and mouse 11β‐HSD1 and are selective with no activity against 11β‐HSD2 and 17β‐HSD1. Selected potent 11β‐HSD1 inhibitors show moderate metabolic stability upon incubation with human liver microsomes and weak inhibition of human CYP450 enzymes." @default.
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- W2035128931 date "2011-05-23" @default.
- W2035128931 modified "2023-10-16" @default.
- W2035128931 title "Discovery of Adamantyl Heterocyclic Ketones as Potent 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitors" @default.
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- W2035128931 doi "https://doi.org/10.1002/cmdc.201100144" @default.
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