• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利：CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法，用中文像聊天一样搜索，搜遍4000万医学文献。AI智能推荐，让科研检索更轻松。

立即免费搜索

文件翻译

保留排版，准确专业，支持PDF/Word/PPT等文件格式，支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述，25分钟生成高质量综述，智能提取关键信息，辅助科研写作。

立即免费体验

相似文献

1
Bifunctional polymeric inhibitors of human influenza A viruses.人甲型流感病毒的双功能聚合抑制剂。
Pharm Res. 2010 Feb;27(2):259-63. doi: 10.1007/s11095-009-0013-1. Epub 2009 Dec 15.
2
Thiosialoside-decorated polymers use a two-step mechanism to inhibit both early and late stages of influenza virus infection.硫代唾液酸修饰聚合物通过两步机制抑制流感病毒感染的早期和晚期阶段。
Eur J Med Chem. 2020 Aug 1;199:112357. doi: 10.1016/j.ejmech.2020.112357. Epub 2020 Apr 28.
3
Attaching zanamivir to a polymer markedly enhances its activity against drug-resistant strains of influenza a virus.将扎那米韦连接到聚合物上显著增强了其对流感 a 病毒耐药株的活性。
J Pharm Sci. 2011 Mar;100(3):831-5. doi: 10.1002/jps.22338. Epub 2010 Aug 25.
4
Conjugation to polymeric chains of influenza drugs targeting M2 ion channels partially restores inhibition of drug-resistant mutants.将流感药物与针对 M2 离子通道的聚合链连接起来，部分恢复了对耐药突变体的抑制作用。
J Pharm Sci. 2013 Aug;102(8):2450-9. doi: 10.1002/jps.23644. Epub 2013 Jul 6.
5
Conjugating drug candidates to polymeric chains does not necessarily enhance anti-influenza activity.将候选药物与聚合物链连接不一定能增强抗流感活性。
J Pharm Sci. 2012 Oct;101(10):3896-905. doi: 10.1002/jps.23253. Epub 2012 Jul 11.
6
Polymer-attached zanamivir inhibits synergistically both early and late stages of influenza virus infection.聚合物连接扎那米韦协同抑制流感病毒感染的早期和晚期阶段。
Proc Natl Acad Sci U S A. 2012 Dec 11;109(50):20385-90. doi: 10.1073/pnas.1219155109. Epub 2012 Nov 26.
7
Dimeric zanamivir conjugates with various linking groups are potent, long-lasting inhibitors of influenza neuraminidase including H5N1 avian influenza.具有各种连接基团的二聚体扎那米韦共轭物是包括H5N1禽流感在内的流感神经氨酸酶的强效、长效抑制剂。
J Med Chem. 2005 Apr 21;48(8):2964-71. doi: 10.1021/jm040891b.
8
Zanamivir conjugated to poly-L-glutamine is much more active against influenza viruses in mice and ferrets than the drug itself.与聚-L-谷氨酰胺缀合的扎那米韦在小鼠和雪貂体内对流感病毒的活性比药物本身高得多。
Pharm Res. 2014 Feb;31(2):466-74. doi: 10.1007/s11095-013-1175-4. Epub 2013 Sep 25.
9
Synthesis and anti-influenza evaluation of polyvalent sialidase inhibitors bearing 4-guanidino-Neu5Ac2en derivatives.携带4-胍基-唾液酸-2-烯丙酯衍生物的多价唾液酸酶抑制剂的合成与抗流感评价
Chem Pharm Bull (Tokyo). 2003 Dec;51(12):1386-98. doi: 10.1248/cpb.51.1386.
10
An M2-V27A channel blocker demonstrates potent in vitro and in vivo antiviral activities against amantadine-sensitive and -resistant influenza A viruses.一种M2-V27A通道阻滞剂对金刚烷胺敏感和耐药的甲型流感病毒均表现出强大的体外和体内抗病毒活性。
Antiviral Res. 2017 Apr;140:45-54. doi: 10.1016/j.antiviral.2017.01.006. Epub 2017 Jan 10.

引用本文的文献

1
Polyvalent Glycan Functionalized Quantum Nanorods as Mechanistic Probes for Shape-Selective Multivalent Lectin-Glycan Recognition.多价聚糖功能化量子纳米棒作为形状选择性多价凝集素-聚糖识别的机制探针。
ACS Appl Nano Mater. 2023 Mar 14;6(6):4201-4213. doi: 10.1021/acsanm.2c05247. eCollection 2023 Mar 24.
2
Design and Functional Analysis of Heterobifunctional Multivalent Phage Capsid Inhibitors Blocking the Entry of Influenza Virus.设计与功能分析的杂双功能多价噬菌体衣壳抑制剂阻断流感病毒的进入。
Bioconjug Chem. 2022 Jul 20;33(7):1269-1278. doi: 10.1021/acs.bioconjchem.2c00166. Epub 2022 Jun 27.
3
Synthetic Glycomacromolecules of Defined Valency, Absolute Configuration, and Topology Distinguish between Human Lectins.具有确定价态、绝对构型和拓扑结构的合成糖大分子可区分人凝集素。
JACS Au. 2021 Aug 10;1(10):1621-1630. doi: 10.1021/jacsau.1c00255. eCollection 2021 Oct 25.
4
Topology-Matching Design of an Influenza-Neutralizing Spiky Nanoparticle-Based Inhibitor with a Dual Mode of Action.具有双重作用模式的流感中和刺状纳米颗粒基抑制剂的拓扑匹配设计
Angew Chem Weinheim Bergstr Ger. 2020 Sep 1;132(36):15662-15666. doi: 10.1002/ange.202004832. Epub 2020 Jul 8.
5
Topology-Matching Design of an Influenza-Neutralizing Spiky Nanoparticle-Based Inhibitor with a Dual Mode of Action.基于刺突纳米颗粒的具有双重作用模式的流感中和抑制剂的拓扑匹配设计。
Angew Chem Int Ed Engl. 2020 Sep 1;59(36):15532-15536. doi: 10.1002/anie.202004832. Epub 2020 Jul 8.
6
Development of effective anti-influenza drugs: congeners and conjugates - a review.抗流感药物的研发：同系物和缀合物——综述。
J Biomed Sci. 2019 Oct 23;26(1):84. doi: 10.1186/s12929-019-0567-0.
7
Advanced Prodrug Strategies in Nucleoside and Non-Nucleoside Antiviral Agents: A Review of the Recent Five Years.核苷类和非核苷类抗病毒药物的高级前药策略：对最近五年的综述。
Molecules. 2017 Oct 16;22(10):1736. doi: 10.3390/molecules22101736.
8
Multivalent Peptide-Nanoparticle Conjugates for Influenza-Virus Inhibition.多价肽-纳米颗粒缀合物抑制流感病毒。
Angew Chem Int Ed Engl. 2017 May 15;56(21):5931-5936. doi: 10.1002/anie.201702005. Epub 2017 Apr 26.
9
Influenza Neuraminidase Inhibitors: Synthetic Approaches, Derivatives and Biological Activity.流感神经氨酸酶抑制剂：合成方法、衍生物及生物活性
Molecules. 2016 Nov 11;21(11):1513. doi: 10.3390/molecules21111513.
10
Zanamivir conjugated to poly-L-glutamine is much more active against influenza viruses in mice and ferrets than the drug itself.与聚-L-谷氨酰胺缀合的扎那米韦在小鼠和雪貂体内对流感病毒的活性比药物本身高得多。
Pharm Res. 2014 Feb;31(2):466-74. doi: 10.1007/s11095-013-1175-4. Epub 2013 Sep 25.

本文引用的文献

1
Polyvalent Interactions in Biological Systems: Implications for Design and Use of Multivalent Ligands and Inhibitors.生物系统中的多价相互作用：对多价配体和抑制剂设计与应用的启示
Angew Chem Int Ed Engl. 1998 Nov 2;37(20):2754-2794. doi: 10.1002/(SICI)1521-3773(19981102)37:20<2754::AID-ANIE2754>3.0.CO;2-3.
2
The war against influenza: discovery and development of sialidase inhibitors.对抗流感之战：唾液酸酶抑制剂的发现与研发
Nat Rev Drug Discov. 2007 Dec;6(12):967-74. doi: 10.1038/nrd2400.
3
Hydrophobic polycationic coatings inactivate wild-type and zanamivir- and/or oseltamivir-resistant human and avian influenza viruses.疏水性聚阳离子涂层可使野生型以及对扎那米韦和/或奥司他韦耐药的人类和禽流感病毒失活。
Biotechnol Lett. 2008 Mar;30(3):475-9. doi: 10.1007/s10529-007-9565-5. Epub 2007 Oct 31.
4
Antiviral agents active against influenza A viruses.对甲型流感病毒有效的抗病毒药物。
Nat Rev Drug Discov. 2006 Dec;5(12):1015-25. doi: 10.1038/nrd2175.
5
Polymeric coatings that inactivate both influenza virus and pathogenic bacteria.能使流感病毒和致病细菌失活的聚合物涂层。
Proc Natl Acad Sci U S A. 2006 Nov 21;103(47):17667-71. doi: 10.1073/pnas.0608803103. Epub 2006 Nov 13.
6
Influenza pandemic periodicity, virus recycling, and the art of risk assessment.流感大流行的周期性、病毒循环及风险评估的技巧
Emerg Infect Dis. 2006 Jan;12(1):34-9. doi: 10.3201/eid1201.051013.
7
Neuraminidase inhibitor-resistant influenza viruses may differ substantially in fitness and transmissibility.对神经氨酸酶抑制剂耐药的流感病毒在适应性和传播性方面可能存在很大差异。
Antimicrob Agents Chemother. 2005 Oct;49(10):4075-84. doi: 10.1128/AAC.49.10.4075-4084.2005.
8
Influenza viruses resistant to the antiviral drug oseltamivir: transmission studies in ferrets.对抗病毒药物奥司他韦耐药的流感病毒：雪貂传播研究
J Infect Dis. 2004 Nov 1;190(9):1627-30. doi: 10.1086/424572. Epub 2004 Sep 28.
9
Synthesis and anti-influenza evaluation of polyvalent sialidase inhibitors bearing 4-guanidino-Neu5Ac2en derivatives.携带4-胍基-唾液酸-2-烯丙酯衍生物的多价唾液酸酶抑制剂的合成与抗流感评价
Chem Pharm Bull (Tokyo). 2003 Dec;51(12):1386-98. doi: 10.1248/cpb.51.1386.
10
Synthesis and anti-influenza evaluation of polyvalent sialidase inhibitors bearing 4-guanidino-Neu5Ac2en derivatives.含4-胍基-唾液酸烯丙酯衍生物的多价唾液酸酶抑制剂的合成及抗流感活性评价
Bioorg Med Chem Lett. 2002 Aug 5;12(15):1929-32. doi: 10.1016/s0960-894x(02)00330-x.

人甲型流感病毒的双功能聚合抑制剂。

Bifunctional polymeric inhibitors of human influenza A viruses.

机构信息

Department of Chemistry, Massachusetts Institute of Technology, Cambridge, Massachusetts 02139, USA.

出版信息

Pharm Res. 2010 Feb;27(2):259-63. doi: 10.1007/s11095-009-0013-1. Epub 2009 Dec 15.

DOI:10.1007/s11095-009-0013-1
PMID:20013036
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2847411/
Abstract

PURPOSE

New antiviral agents were prepared by attaching derivatives of sialic acid (1) and of the drug zanamivir (2) to poly(isobutylene-alt-maleic anhydride) (poly-(1 + 2)) or by mixing poly-1 and poly-2, followed by assaying them against wild-type and drug-resistant influenza A Wuhan viruses.

METHODS

Individually or together, 1 and 2 were covalently bonded to the polymer. The antiviral potencies of the resultant poly-1, poly-2, poly-(1 + 2), and poly-1 + poly-2, as well as 1 and 2, were assessed using plaque reduction assay.

RESULTS

Attaching 1 to the polymer improved at best millimolar IC(50) values over three orders of magnitude. While 2 exhibited micromolar IC(50) values, poly-2 was >100-fold even more potent. The IC(50) of poly-(1 + 2) against the wild-type strain was >300-fold and approximately 17-fold better than of poly-1 and poly-2, respectively. In contrast, the potency of poly-(1 + 2) vs. poly-2 against the mutant strain merely doubled. The mixture of poly-1 + poly-2 inhibited both viral strains similarly to poly-2.

CONCLUSIONS

The bifunctional poly-(1 + 2) acts synergistically against the wild-type influenza virus, but not against its drug-resistant mutant, as compared to a physical mixture of the monofunctional poly-1 and poly-2.

摘要

目的

通过将唾液酸（1）和扎那米韦（2）的衍生物连接到聚异丁烯-马来酸酐共聚物（聚（1+2））或混合聚（1）和聚（2），然后对其进行抗野生型和耐药型流感 A 武汉病毒的检测，制备了新的抗病毒药物。

方法

1 和 2 分别或一起与聚合物共价结合。通过噬菌斑减少法评估所得的聚（1）、聚（2）、聚（1+2）和聚（1+2）以及 1 和 2 的抗病毒效力。

结果

将 1 连接到聚合物上可将最佳毫摩尔 IC50 值提高三个数量级以上。虽然 2 表现出微摩尔 IC50 值，但聚（2）的效力高 100 倍以上。聚（1+2）对野生型菌株的 IC50 值>300 倍，分别比聚（1）和聚（2）高约 17 倍。相比之下，聚（1+2）对突变株的效力仅提高了两倍。聚（1+2）混合物对两种病毒株的抑制作用与聚（2）相似。

结论

与单功能聚（1）和聚（2）的物理混合物相比，双功能聚（1+2）对野生型流感病毒具有协同作用，但对其耐药突变体则没有。