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1.
Bioorg Med Chem Lett ; 22(9): 3291-5, 2012 May 01.
Article in English | MEDLINE | ID: mdl-22465636

ABSTRACT

The introduction of A ring pyrazole modification to the hydrocortisone C-21 heteroaryl thioethers generated compounds with excellent transrepression potency (IL-8 inhibition) compared to their hydrocortisone analogs. However, the transcriptional transactivation activity of these compounds were considerably higher than the corresponding hydrocortisone analogs. Among all the compounds evaluated, a quinoxaline thioether modification demonstrated the best overall in vitro separation.


Subject(s)
Receptors, Glucocorticoid/drug effects , Steroids/chemistry , Sulfides/chemistry , Humans , Hydrocortisone , Pyrazoles/chemistry , Structure-Activity Relationship , Sulfides/pharmacology , Transcriptional Activation/drug effects
2.
Bioorg Med Chem Lett ; 22(2): 1086-90, 2012 Jan 15.
Article in English | MEDLINE | ID: mdl-22197391

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.


Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Drug Discovery , Receptors, Glucocorticoid/agonists , Sulfides/pharmacology , Administration, Oral , Animals , Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Anti-Inflammatory Agents, Non-Steroidal/chemistry , Biological Availability , Cell Line , Dose-Response Relationship, Drug , Hep G2 Cells , Humans , Molecular Conformation , Rats , Rats, Inbred BN , Receptors, Glucocorticoid/metabolism , Stereoisomerism , Structure-Activity Relationship , Sulfides/administration & dosage , Sulfides/chemistry , Tyrosine Transaminase/metabolism
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