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Steroidal C-21 heteroaryl thioethers (Part 2): discovery of orally bioavailable selective glucocorticoid receptor modulators (dissociated steroids) |
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| Authors: | Biju Purakkattle McCormick Kevin Aslanian Robert Berlin Michael Solomon Daniel Wang Hongwu Lee Yoon Joo Bitar Rema Prelusky Daniel McLeod Robbie Jia Yanlin Fernandez Xiomora Eckel Stephen House Aileen Lieber Gissela Jimenez Johanna Kelly George Chapman Richard Phillips Jonathan Anthes John |
| Affiliation: | Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, USA. purakkattle.biju@merck.com |
| 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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