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

  title={Design and optimisation of orally active TLR7 agonists for the treatment of hepatitis C virus infection.},
  author={T. Tran and D. Pryde and Peter Jones and F. Adam and N. Benson and G. Bish and F. Calo and G. Ciaramella and R. Dixon and Jonathan Duckworth and D. Fox and D. Hay and James R. Hitchin and N. Horscroft and Martin Howard and I. Gardner and H. Jones and C. Laxton and T. Parkinson and Gemma C. Parsons and Katie J. W. Proctor and Mya C. Smith and Nicholas N. Smith and A. Thomas},
  journal={Bioorganic \& medicinal chemistry letters},
  volume={21 8},
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. 
Discovery of a highly potent series of TLR7 agonists.
Interferons as Therapeutic Agents for Infectious Diseases
Latest Advances in Small Molecule TLR 7/8 Agonist Drug Research.
Conjugation of a TLR7 agonist and antigen enhances protection in the S. pneumoniae murine infection model.
  • S. Vecchi, S. Bufali, +5 authors D. O'hagan
  • Biology, Medicine
  • European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V
  • 2014
Strategies for designing synthetic immune agonists
  • T. Wu
  • Biology, Medicine
  • Immunology
  • 2016
Design and Synthesis of a New Soluble Natural β-Carboline Derivative for Preclinical Study by Intravenous Injection


Molecular basis for the immunostimulatory activity of guanine nucleoside analogs: Activation of Toll-like receptor 7
The antiviral activity of Toll-like receptor 7 and 7/8 agonists.
Imiquimod and resiquimod as novel immunomodulators.
Imiquimod as a dermatological therapy
Aldehyde oxidase: an enzyme of emerging importance in drug discovery.