| Literature DB >> 21944381 |
Purakkattle Biju1, Kevin McCormick, Robert Aslanian, Michael Berlin, Daniel Solomon, Richard Chapman, Robbie McLeod, Daniel Prelusky, Stephen Eckel, George Kelly, Michelle Natiello, Aileen House, Xiomara Fernandez, Rema Bitar, Jonathan Phillips, John Anthes.
Abstract
A series of C-21 mercapto derivatives of hydrocortisone have been synthesized and evaluated in cell based transrepression and transactivation assays. The benzothiazole derivative, compound 6 not only showed a dissociated profile in vitro functional assays but also a pharmacological profile in a Brown-Norway rat therapeutic index model of asthma that dissociated side effects (thymolysis) while maintaining efficacy against pulmonary inflammation and lung function.Entities:
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Year: 2011 PMID: 21944381 DOI: 10.1016/j.bmcl.2011.08.108
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN: 0960-894X Impact factor: 2.823