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Published on: April 6, 2017
Steroidal C-21 mercapto derivatives as dissociated steroids: discovery of an inhaled dissociated steroid
Purakkattle Biju1, Kevin McCormick, Robert Aslanian
1Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. julianbiju@yahoo.com
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.
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