Abstract
2,5,5-Trisubstituted oxazolones were identified as potent inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1). The synthesis, structure-activity relationship and metabolic stability of these compounds are presented.
MeSH terms
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11-beta-Hydroxysteroid Dehydrogenase Type 1 / antagonists & inhibitors*
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Animals
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Chemistry, Pharmaceutical / methods*
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Cortisone / chemistry
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Drug Design
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Drug Evaluation, Preclinical
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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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Humans
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Hydrocortisone / chemistry
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Models, Chemical
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Oxazoles / pharmacology*
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Rats
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Structure-Activity Relationship
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Thiazoles / chemistry
Substances
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Enzyme Inhibitors
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Oxazoles
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Thiazoles
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11-beta-Hydroxysteroid Dehydrogenase Type 1
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Cortisone
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Hydrocortisone