Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10595279 | Bioorganic & Medicinal Chemistry Letters | 2012 | 5 Pages |
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.
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Authors
Purakkattle Biju, Kevin McCormick, Robert Aslanian, Michael Berlin, Daniel Solomon, Hongwu Wang, Yoon Joo Lee, Rema Bitar, Daniel Prelusky, Robbie Mcleod, Yanlin Jia, Xiomora Fernandez, Stephen Eckel, Aileen House, Gissela Lieber, Johanna Jimenez,