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烯基取代的双环核苷类似物对水痘带状疱疹病毒仍保持纳摩尔级别的效力。

Alkenyl substituted bicyclic nucleoside analogues retain nanomolar potency against Varicella Zoster Virus.

作者信息

McGuigan Christopher, Bidet Olivier, Derudas Marco, Andrei Graciela, Snoeck Robert, Balzarini Jan

机构信息

Welsh School of Pharmacy, Cardiff University, Redwood Building, King Edward VII Avenue, Cardiff CF10 3NB, UK.

出版信息

Bioorg Med Chem. 2009 Apr 15;17(8):3025-7. doi: 10.1016/j.bmc.2009.03.022. Epub 2009 Mar 14.

DOI:10.1016/j.bmc.2009.03.022
PMID:19328697
Abstract

Novel alkenyl substituted aryl bicyclic furano pyrimidines have been prepared and evaluated in vitro against Varicella Zoster Virus (VZV). The para-substituted analogues retain the nanomolar potency we have reported for p-alkyl analogues, while the ortho- and meta-alkenyl systems lose 3-4 orders of potency.

摘要

新型烯基取代的芳基双环呋喃嘧啶已被制备并在体外针对水痘带状疱疹病毒(VZV)进行了评估。对位取代的类似物保留了我们报道的对烷基类似物的纳摩尔效力,而邻位和间位烯基系统的效力则降低了3 - 4个数量级。

相似文献

1
Alkenyl substituted bicyclic nucleoside analogues retain nanomolar potency against Varicella Zoster Virus.烯基取代的双环核苷类似物对水痘带状疱疹病毒仍保持纳摩尔级别的效力。
Bioorg Med Chem. 2009 Apr 15;17(8):3025-7. doi: 10.1016/j.bmc.2009.03.022. Epub 2009 Mar 14.
2
Bicyclic nucleoside inhibitors of varicella-zoster virus (VZV): effect of terminal unsaturation in the side-chain.水痘带状疱疹病毒(VZV)的双环核苷抑制剂:侧链末端不饱和的影响。
Nucleosides Nucleotides Nucleic Acids. 2001 Apr-Jul;20(4-7):763-6. doi: 10.1081/NCN-100002425.
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Bicyclic anti-VZV nucleosides: thieno analogues bearing an alkylphenyl side chain have reduced antiviral activity.双环抗水痘带状疱疹病毒核苷:带有烷基苯基侧链的噻吩类似物抗病毒活性降低。
Bioorg Med Chem Lett. 2004 May 17;14(10):2397-9. doi: 10.1016/j.bmcl.2004.03.029.
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Bicyclic nucleoside inhibitors of Varicella-Zoster virus: the effect of branching in the p-alkylphenyl side chain.水痘-带状疱疹病毒的双环核苷抑制剂:对-烷基苯基侧链中支链的影响
Bioorg Med Chem Lett. 2005 Aug 15;15(16):3791-6. doi: 10.1016/j.bmcl.2005.05.071.
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Bicyclic nucleoside inhibitors of Varicella-Zoster Virus (VZV): the effect of terminal unsaturation in the side chain.
Bioorg Med Chem Lett. 2001 Feb 12;11(3):391-3. doi: 10.1016/s0960-894x(00)00672-7.
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Highly potent and selective inhibition of varicella-zoster virus by bicyclic furopyrimidine nucleosides bearing an aryl side chain.带有芳基侧链的双环呋嘧啶核苷对水痘带状疱疹病毒具有高效且选择性的抑制作用。
J Med Chem. 2000 Dec 28;43(26):4993-7. doi: 10.1021/jm000210m.
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Synthesis and antiviral activity of the carbocyclic analogue of the highly potent and selective anti-VZV bicyclo furano pyrimidines.高效且选择性抗水痘带状疱疹病毒双环呋喃嘧啶的碳环类似物的合成及抗病毒活性
J Med Chem. 2007 Dec 27;50(26):6485-92. doi: 10.1021/jm070357e. Epub 2007 Dec 6.
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Metabolic and pharmacological characteristics of the bicyclic nucleoside analogues (BCNAs) as highly selective inhibitors of varicella-zoster virus (VZV).双环核苷类似物(BCNAs)作为水痘带状疱疹病毒(VZV)高度选择性抑制剂的代谢和药理学特性。
Nucleosides Nucleotides Nucleic Acids. 2003 May-Aug;22(5-8):995-7. doi: 10.1081/NCN-120022721.
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Bicyclic nucleoside inhibitors of varicella-zoster virus: synthesis and biological evaluation of 2',3'-dideoxy-3'-fluoro and 2'-deoxy-xylo derivatives.
Nucleosides Nucleotides Nucleic Acids. 2003 May-Aug;22(5-8):935-7. doi: 10.1081/NCN-120022689.
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Bicyclic furo pyrimidine nucleosides with aryloxyphenyl and halophenyl substituted side chains as potent and selective varicella-zoster virus inhibitors.
Nucleosides Nucleotides Nucleic Acids. 2001 Apr-Jul;20(4-7):1063-6. doi: 10.1081/NCN-100002492.

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