Abstract
A series of adamantyl amide 11beta-HSD1 inhibitors has been discovered and chemically modified. Selected compounds are selective for 11beta-HSD1 over 11beta-HSD2 and possess excellent cellular potency in human and murine 11beta-HSD1 assays. Good pharmacodynamic characteristics are observed in ex vivo assays.
Publication types
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Evaluation Study
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Research Support, Non-U.S. Gov't
MeSH terms
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11-beta-Hydroxysteroid Dehydrogenase Type 1 / antagonists & inhibitors*
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11-beta-Hydroxysteroid Dehydrogenase Type 2 / antagonists & inhibitors
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Adamantane / analogs & derivatives*
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Adamantane / chemistry
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Adamantane / pharmacology*
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Amides / chemistry
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Amides / pharmacology*
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Animals
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology*
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Humans
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Mice
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Molecular Structure
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Structure-Activity Relationship
Substances
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Amides
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Enzyme Inhibitors
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11-beta-Hydroxysteroid Dehydrogenase Type 1
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11-beta-Hydroxysteroid Dehydrogenase Type 2
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Adamantane