Design and optimisation of orally active TLR7 agonists for the treatment of hepatitis C virus infection

Autor:	Carl Laxton, Nicholas Smith, Martin Howard, Gerwyn Bish, Duncan Hay, Mya C. Smith, James Hitchin, Tram T. Tran, David C. Pryde, Hannah M. Jones, Peter Jones, Nigel Horscroft, Gemma C. Parsons, Rachel Dixon, Frederick Calo, Katie J. W. Proctor, Fox David Nathan Abraham, Jonathan Duckworth, Neil Benson, Amy Thomas, Iain Gardner, Tanya Parkinson, Fiona M. Adam, Guiseppe Ciaramella
Rok vydání:	2011
Předmět:	Agonist medicine.drug_class Hepacivirus Hepatitis C virus Clinical Biochemistry Administration Oral Pharmaceutical Science Pharmacology medicine.disease_cause Antiviral Agents Biochemistry Virus Mice Structure-Activity Relationship RNA Virus Infections In vivo Drug Discovery medicine Animals Structure–activity relationship Molecular Biology Interferon inducer biology Chemistry Organic Chemistry TLR7 biology.organism_classification Rats Toll-Like Receptor 7 Purines Drug Design Models Animal Immunology Molecular Medicine
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 21:2389-2393
ISSN:	0960-894X
Popis:	The 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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ca3f64c50e8a92b29c2e40cbf07d158d https://doi.org/10.1016/j.bmcl.2011.02.092 Zobrazit plný text záznamu Full Text from ScienceDirect