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Design and optimisation of orally active TLR7 agonists for the treatment of hepatitis C virus infection |
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| Authors: | Tran Thien-Duc Pryde David C Jones Peter Adam Fiona M Benson Neil Bish Gerwyn Calo Frederick Ciaramella Guiseppe Dixon Rachel Duckworth Jonathan Fox David N A Hay Duncan A Hitchin James Horscroft Nigel Howard Martin Gardner Iain Jones Hannah M Laxton Carl Parkinson Tanya Parsons Gemma Proctor Katie Smith Mya C Smith Nicholas Thomas Amy |
| Affiliation: | a Discovery Chemistry, Dynamics and Metabolism, Pfizer Global Research and Development, Sandwich Laboratories, Ramsgate Road, Sandwich, Kent, CT13 9NJ, UK b Discovery Biology, Dynamics and Metabolism, Pfizer Global Research and Development, Sandwich Laboratories, Ramsgate Road, Sandwich, Kent, CT13 9NJ, UK c Department of Pharmacokinetics, Dynamics and Metabolism, Pfizer Global Research and Development, Sandwich Laboratories, Ramsgate Road, Sandwich, Kent, CT13 9NJ, UK d SRG, London Office, 16, St. Helen’s place, London, EC3A 6DF, UK |
| 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. |
| Keywords: | TLR7 agonist HCV Interferon inducer Aldehyde oxidase |
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