Abstract
A series of novel corticosteroid derivatives featuring C-17 furoate ester functionality have been synthesised. Profiling in vitro and in vivo has resulted in the identification of a compound with a longer duration of action and a lower oral side effect profile in rodents compared to budesonide.
MeSH terms
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Androstenes / chemical synthesis*
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Androstenes / pharmacokinetics
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Androstenes / pharmacology
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Animals
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Biological Availability
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Cell Line
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Eosinophilia / drug therapy
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Esters / chemical synthesis*
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Esters / pharmacokinetics
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Esters / pharmacology
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Glucocorticoids / chemical synthesis*
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Glucocorticoids / pharmacokinetics
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Glucocorticoids / pharmacology
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Humans
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Macrophages / cytology
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Organ Size / drug effects
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Protein Binding
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Rats
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Receptors, Glucocorticoid / agonists*
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Structure-Activity Relationship
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Thymus Gland / drug effects
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Tumor Necrosis Factor-alpha / analysis
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Tumor Necrosis Factor-alpha / antagonists & inhibitors
Substances
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Androstenes
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Esters
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Glucocorticoids
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Receptors, Glucocorticoid
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Tumor Necrosis Factor-alpha