Issue 3, 2011
From the journal:

MedChemComm

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

David C. Pryde,*a   Thien-Duc Tran,a   Peter Jones,a   Gemma C. Parsons,a   Gerwyn Bish,a   Fiona M. Adam,a   Mya C. Smith,a   Donald S. Middleton,a   Nick N. Smith,a   Frederick Calo,a   Duncan Hay,a   Michael Paradowski,a   Katie J. W. Proctor,a   Tanya Parkinson,b   Carl Laxton,b   David N. A. Fox,a   Nigel J. Horscroft,b   Giuseppe Ciaramella,b   Hannah M. Jones,c   Jonathan Duckworth,c   Neil Benson,c   Anthony Harrisonc  and  Rob Websterc  

* Corresponding authors

a WorldWide Medicinal Chemistry, Pfizer Global Research and Development, Ramsgate Road, Sandwich, Kent, England
E-mail: David.Pryde@pfizer.com
Tel: +44(1304) 643687

b Discovery Biology, Pfizer Global Research and Development, Ramsgate Road, Sandwich, Kent, England

c Pharmacokinetics, Dynamics and Metabolism, Pfizer Global Research and Development, Ramsgate Road, Sandwich, Kent, England

Abstract

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.

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

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Article information

DOI
https://doi.org/10.1039/C0MD00197J
Article type
Concise Article
Submitted
01 Nov 2010
Accepted
03 Dec 2010
First published
20 Dec 2010

Med. Chem. Commun., 2011,2, 185-189

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

D. C. Pryde, T. Tran, P. Jones, G. C. Parsons, G. Bish, F. M. Adam, M. C. Smith, D. S. Middleton, N. N. Smith, F. Calo, D. Hay, M. Paradowski, K. J. W. Proctor, T. Parkinson, C. Laxton, D. N. A. Fox, N. J. Horscroft, G. Ciaramella, H. M. Jones, J. Duckworth, N. Benson, A. Harrison and R. Webster, Med. Chem. Commun., 2011, 2, 185 DOI: 10.1039/C0MD00197J

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