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TitleDesign and optimisation of orally active TLR7 agonists for the treatment of hepatitis C virus infection
Publication TypeJournal Article
Year of Publication2011
AuthorsTran, T.-D., Pryde D.C., Jones P., Adam F.M., Benson N., Bish G., Calo F., Ciaramella G., Dixon R., Duckworth J., Fox D.N.A., Hay D.A., Hitchin J., Horscroft N., Howard M., Gardner I., Jones H.M., Laxton C., Parkinson T., Parsons G., Proctor K., Smith M.C., Smith N., and Thomas A.
JournalBioorganic and Medicinal Chemistry Letters
Pagination2389 - 2393
Date Published2011
ISSN0960894X (ISSN)
KeywordsAdministration, Oral, animal cell, animal experiment, Animals, Antiviral Agents, article, drug absorption, drug design, drug distribution, drug efficacy, drug elimination, drug half life, drug potency, drug selectivity, drug solubility, drug stability, drug synthesis, Hepacivirus, hepatitis C, Hepatitis C virus, human, human cell, interferon induction, liver microsome, Mice, Models, Animal, mouse, nonhuman, process optimization, Purines, rat, Rats, RNA Virus Infections, structure activity relation, Structure-Activity Relationship, tetrahydropyran derivative, toll like receptor 7, toll like receptor agonist, Toll-Like Receptor 7
AbstractThe synthesis and structure-activity relationships of a series of novel interferon inducers are described. Pharmacokinetic studies and efficacy assessment of a series of 8-oxo-3-deazapurine analogues led to the identification of compound 33, a potent and selective agonist of the TLR7 receptor with an excellent in vivo efficacy profile in a mouse model. © 2011 Elsevier Ltd. All rights reserved.

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