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Bioorg Med Chem Lett. 2012 Jan 15;22(2):1086-90. doi: 10.1016/j.bmcl.2011.11.120. Epub 2011 Dec 7.

Steroidal C-21 heteroaryl thioethers (Part 2): discovery of orally bioavailable selective glucocorticoid receptor modulators (dissociated steroids).

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  • 1Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, USA.


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.

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