Abstract
The prednisolone C-21 heteroaryl thioethers have been synthesized and evaluated in cell based transrepression and transactivation assays. Most of the compounds demonstrated weak transactivational activity in both human and rat tyrosineaminotransferase functional assay while keeping potent anti-inflammatory activity. The benzimidazole thioether 7 exhibited comparable anti-inflammatory activity and improved safety profile compared to the classical oral steroid prednisolone.
Copyright © 2011 Elsevier Ltd. All rights reserved.
MeSH terms
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Administration, Oral
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Animals
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Anti-Inflammatory Agents, Non-Steroidal / administration & dosage
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Anti-Inflammatory Agents, Non-Steroidal / chemistry
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Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
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Biological Availability
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Cell Line
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Dose-Response Relationship, Drug
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Drug Discovery*
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Hep G2 Cells
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Humans
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Molecular Conformation
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Rats
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Rats, Inbred BN
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Receptors, Glucocorticoid / agonists*
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Receptors, Glucocorticoid / metabolism
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Stereoisomerism
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Structure-Activity Relationship
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Sulfides / administration & dosage
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Sulfides / chemistry
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Sulfides / pharmacology*
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Tyrosine Transaminase / metabolism
Substances
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Anti-Inflammatory Agents, Non-Steroidal
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Receptors, Glucocorticoid
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Sulfides
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Tyrosine Transaminase