Document Detail


Steroidal C-21 mercapto derivatives as dissociated steroids: Discovery of an inhaled dissociated steroid.
MedLine Citation:
PMID:  21944381     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
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.
Authors:
Purakkattle Biju; 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
Publication Detail:
Type:  -     Date:  2011-8-31
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  -     ISSN:  1464-3405     ISO Abbreviation:  -     Publication Date:  2011 Aug 
Date Detail:
Created Date:  2011-9-27     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
Copyright © 2011 Elsevier Ltd. All rights reserved.
Affiliation:
Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
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