Literature DB >> 21419626

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

Thien-Duc Tran1, David C Pryde, Peter Jones, Fiona M Adam, Neil Benson, Gerwyn Bish, Frederick Calo, Guiseppe Ciaramella, Rachel Dixon, Jonathan Duckworth, David N A Fox, Duncan A Hay, James Hitchin, Nigel Horscroft, Martin Howard, Iain Gardner, Hannah M Jones, Carl Laxton, Tanya Parkinson, Gemma Parsons, Katie Proctor, Mya C Smith, Nicholas Smith, Amy Thomas.   

Abstract

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.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID: 21419626     DOI: 10.1016/j.bmcl.2011.02.092

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  5 in total

Review 1.  Strategies for designing synthetic immune agonists.

Authors:  Tom Y-H Wu
Journal:  Immunology       Date:  2016-07-11       Impact factor: 7.397

Review 2.  Interferons as therapeutic agents for infectious diseases.

Authors:  Scott J Bergman; McKenzie C Ferguson; Cathy Santanello
Journal:  Infect Dis Clin North Am       Date:  2011-12       Impact factor: 5.982

3.  Discovery of new TLR7 agonists by a combination of statistical learning-based QSAR, virtual screening, and molecular dynamics.

Authors:  Ardavan Abiri; Masoud Rezaei; Mohammad Hossein Zeighami; Younes Vaezpour; Leili Dehghan; Maedeh KhorramGhahfarokhi
Journal:  Inform Med Unlocked       Date:  2021-11-15

Review 4.  Structural evolution of toll-like receptor 7/8 agonists from imidazoquinolines to imidazoles.

Authors:  Deepender Kaushik; Arshpreet Kaur; Nikolai Petrovsky; Deepak B Salunke
Journal:  RSC Med Chem       Date:  2021-05-14

5.  Toll-like receptor 7 agonists: chemical feature based pharmacophore identification and molecular docking studies.

Authors:  Hui Yu; Hongwei Jin; Lidan Sun; Liangren Zhang; Gang Sun; Zhanli Wang; Yongchun Yu
Journal:  PLoS One       Date:  2013-03-20       Impact factor: 3.240

  5 in total

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