The discovery of a novel prototype small molecule TLR7 agonist for the treatment of hepatitis C virus infection

A series of heterocycle analogues of an adenine template were explored for TLR7 agonist potency and pharmacokinetics. One compound was identified with an excellent pharmacokinetic, in vitro potency and in vivo interferon induction profile in a mouse model, and was selected for further pre-clinical e...

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Veröffentlicht in:MedChemComm 2011-03, Vol.2 (3), p.185-189
Hauptverfasser: Pryde, David C., Tran, Thien-Duc, Jones, Peter, Parsons, Gemma C., Bish, Gerwyn, Adam, Fiona M., Smith, Mya C., Middleton, Donald S., Smith, Nick N., Calo, Frederick, Hay, Duncan, Paradowski, Michael, Proctor, Katie J. W., Parkinson, Tanya, Laxton, Carl, Fox, David N. A., Horscroft, Nigel J., Ciaramella, Giuseppe, Jones, Hannah M., Duckworth, Jonathan, Benson, Neil, Harrison, Anthony, Webster, Rob
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Sprache:eng
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Zusammenfassung:A series of heterocycle analogues of an adenine template were explored for TLR7 agonist potency and pharmacokinetics. One compound was identified with an excellent pharmacokinetic, in vitro potency and in vivo interferon induction profile in a mouse model, and was selected for further pre-clinical evaluation as a potential treatment for hepatitis C viral infection.
ISSN:2040-2503
2040-2511
DOI:10.1039/C0MD00197J