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

被引：16

作者：

Pryde, David C. ^{[1
]}

Tran, Thien-Duc ^{[1
]}

Jones, Peter ^{[1
]}

Parsons, Gemma C. ^{[1
]}

Bish, Gerwyn ^{[1
]}

Adam, Fiona M. ^{[1
]}

Smith, Mya C. ^{[1
]}

Middleton, Donald S. ^{[1
]}

Smith, Nick N. ^{[1
]}

Calo, Frederick ^{[1
]}

Hay, Duncan ^{[1
]}

Paradowski, Michael ^{[1
]}

Proctor, Katie J. W. ^{[1
]}

Parkinson, Tanya ^{[2
]}

Laxton, Carl ^{[2
]}

Fox, David N. A. ^{[1
]}

Horscroft, Nigel J. ^{[2
]}

Ciaramella, Giuseppe ^{[2
]}

Jones, Hannah M. ^{[3
]}

Duckworth, Jonathan ^{[3
]}

Benson, Neil ^{[3
]}

Harrison, Anthony ^{[3
]}

Webster, Rob ^{[3
]}

机构：

[1] Pfizer Global Res & Dev, WorldWide Med Chem, Sandwich CT13 9NJ, Kent, England

[2] Pfizer Global Res & Dev, Discovery Biol, Sandwich CT13 9NJ, Kent, England

[3] Pfizer Global Res & Dev, Pharmacokinet Dynam & Metab, Sandwich CT13 9NJ, Kent, England

来源：

MEDCHEMCOMM | 2011年 / 2卷 / 03期

关键词：

TOLL-LIKE RECEPTORS;

D O I：

10.1039/c0md00197j

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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.

引用

页码：185 / 189

页数：5

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