6677-96-9Relevant articles and documents
Steroidal C-21 mercapto derivatives as dissociated steroids: Discovery of an inhaled dissociated steroid
Biju, Purakkattle,McCormick, Kevin,Aslanian, Robert,Berlin, Michael,Solomon, Daniel,Chapman, Richard,McLeod, Robbie,Prelusky, Daniel,Eckel, Stephen,Kelly, George,Natiello, Michelle,House, Aileen,Fernandez, Xiomara,Bitar, Rema,Phillips, Jonathan,Anthes, John
scheme or table, p. 6343 - 6347 (2011/12/02)
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.
C-21 THIOETHERS AS GLUCOCORTICOID RECEPTOR AGONISTS
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Page/Page column 43, (2009/08/14)
The present invention provides compounds of Formula (VII) and 11-keto analogs thereof, and pharmaceutically acceptable salts, solvates, esters, prodrugs, tautomers, and isomers of said compounds and said 11-keto analogs, having the general structure formula (VII): wherein L, R1, R2, R3, R4, and R5 are selected independently of each other and as defined herein. Also provided are pharmaceutical compositions, methods of preparing, and methods of using such compounds in the treatment and prophylaxis of a wide range of immune, autoimmune, and inflammatory diseases and conditions. The novel compounds of the present invention possess useful pharmacological activity while having unexpectedly low systemic activiy. Thus, the compounds of the invention represent a safer alternative to those known glucocorticoids which have poor side-effect profiles.
SYNTHESIS OF 21-ESTERS OF HYDROCORTISONE WITH GLYCINE AND GLUTAMIC ACID AND STUDY OF THEIR PHARMACOLOGICAL ACTIVITY
Ryakhovskaya, M. I.,Popova, E. V.,Grinenko, G. S.,Terekhina, A. I.,Gritsina, G. I.,et al.
, p. 184 - 189 (2007/10/02)
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