Abstract
A series of metabolically stable adamantane amide 11beta-HSD1 inhibitors have been synthesized and biologically evaluated. These compounds exhibit excellent HSD1 potency and HSD2 selectivity and good pharmacokinetic and pharmacodynamic profiles.
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 / chemical synthesis*
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Adamantane / chemistry
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Adamantane / pharmacology*
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Animals
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Cell Line
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Drug Evaluation, Preclinical
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Enzyme Activation / drug effects
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology*
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Heterocyclic Compounds / chemical synthesis
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Heterocyclic Compounds / chemistry
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Heterocyclic Compounds / pharmacology
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Humans
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In Vitro Techniques
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Mice
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Microsomes, Liver / drug effects
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Microsomes, Liver / enzymology
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Molecular Conformation
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Enzyme Inhibitors
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Heterocyclic Compounds
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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