New hepatitis C drug

StephenW

New hepatitis C drug
http://www.rsc.org/chemistryworld/News/2011/February/14021101.asp
14 February 2011

Scientists in the UK have developed a compound to combat the hepatitis C virus that could be taken as a pill.
DavidPryde and his team from Pfizer Global Research and Development,Sandwich, have made new compounds to activate a protein in the immunesystem called TLR7 - toll-like receptor 7 - which fights the infection.Toll-like receptors identify foreign DNA, such as a virus, and produceproteins that inhibit the virus' replication.
300 million peoplesuffer from hepatitis C worldwide. The virus that causes the diseaseresides in the liver and can lead to cirrhosis, with some sufferersrequiring liver transplants. Current treatments only cure half ofpatients and are administered intravenously. Recent research hasfocused on increasing the effectiveness of the drugs and on developingoral treatments.
Pryde's team made heterocyclic analogues basedon the structure of purines, known activators of TLR7 and the basis ofcurrent oral drugs. 'The most potent TLR7 agonists are purine-based,'explains Pryde. 'But we wanted to design potent non-purine basedagonists to maximise the chances of avoiding any unwanted off-targetpharmacology.'

The compounds activate a protein in the immune system, which fights hepatitis C

Whenthey tested the compounds against a hepatitis C cell line, the teamfound that one of the compounds, a trifluoromethyl derivative, washighly selective for TLR7. The agonist also had comparable performanceto injected alternatives at doses below 50mg.
'Medicinalchemistry is often castigated for surrendering synthetic elegance inorder to gain compound access. Pryde elegantly repudiates this,accomplishing both elegance and access,' says Adam McCluskey, an expertin drug design and discovery from the University of Newcastle,Australia.
Pryde and his team hope to make the agonist more soluble and to increase its potency further before moving on to human trials.
Catherine Bacon

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Link to journal articleThe discovery of a novel prototype small molecule TLR7 agonist for the treatment of hepatitis C virus infection
DavidC. Pryde, Thien-Duc Tran, Peter Jones, Gemma C. Parsons, Gerwyn Bish,Fiona M. Adam, Mya C. Smith, Donald S. Middleton, Nick N. Smith,Frederick Calo, Duncan Hay, Michael Paradowski, Katie J. W. Proctor,Tanya Parkinson, Carl Laxton, David N. A. Fox, Nigel J. Horscroft,Giuseppe Ciaramella, Hannah M. Jones, Jonathan Duckworth, Neil Benson,Anthony Harrison and Rob Webster, Med. Chem. Commun., 2011
DOI: 10.1039/c0md00197j

丙型肝炎的新药物

2011年2月14日

英国科学家已经开发出一种化合物，以打击丙型肝炎病毒，可作为药丸采取的。

大卫和他的普赖德从辉瑞全球研究和开发，夹心队，取得了新的化合物，以激活免疫系统中的一个叫做TLR7蛋白 - Toll样受体7 - 这打架感染。 Toll样受体识别，如外源DNA病毒，并产生蛋白质，抑制病毒复制。

3.00亿人患有丙型肝炎全球。这种病毒是导致这种疾病的驻留在肝脏，可导致肝硬化，肝移植一些需要患者。目前的治疗治愈的病人只有一半，而且是静脉注射。最近的研究侧重于提高了药物的有效性和发展口服治疗。

普赖德的研究小组作出的嘌呤结构，TLR7已知的激活和目前口服药物的基础之上杂环类化合物。 '最有力的TLR7激动剂嘌呤为基础，'解释普赖德。 '但我们想设计有效的非嘌呤受体激动剂的最大化，避免任何不必要的脱靶药理学的机会。'

丙型肝炎的新药物
该化合物在激活免疫系统的蛋白质，打架丙型肝炎

当他们针对丙型肝炎检测细胞系的化合物，该研究小组发现，该化合物，三氟甲基衍生物，一个是高度选择性的TLR7。激动剂也低于50毫克剂量的注射性能媲美的替代品。

湖北医药化学常常受到惩处优雅交出合成化合物，从而获得访问。普赖德优雅否定这一点，实现既优雅和访问，'亚当麦克斯基说，在药物设计专家，来自纽卡斯尔大学，澳大利亚发现。

普赖德和他的团队希望让更多的可溶性受体激动剂和增加，才进入人体试验其效力进一步。

凯瑟琳培根



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链接到期刊文章

对于C型肝炎病毒感染的治疗发现一种新的原型小分子激动剂TLR7
与David C.普赖德，承天，德陈，彼得琼斯，杰玛三帕森斯，Gerwyn比什，菲奥娜米亚当，妙C.史密斯，唐纳德学米德尔顿，尼克史密斯全，冯检基卡洛，邓肯干草，迈克尔Paradowski，凯蒂JW普罗克托中，Tanya帕金森，卡尔拉克斯顿，大卫福克斯北美，奈杰尔j的Horscroft，朱塞佩Ciaramella，汉娜米琼斯，乔纳森达克沃思，尼尔本森，安东尼哈里森和Rob韦伯斯特，地中海。化学。 Commun。，2011
分类号：10.1039/c0md00197j




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HUNHUN2010

多谢就是不知几时才能上市

StephenW

回复 HUNHUN2010 的帖子

很难知道.我不是专家.我相信至少2 -3年.