• 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

六对1,2,4,5-四氧杂环己烷(过氧化物二聚体)和1,2,4,5,7,8-六氧杂环辛烷(过氧化物三聚体)的抗疟活性比较

Comparative antimalarial activities of six pairs of 1,2,4,5-tetraoxanes (peroxide dimers) and 1,2,4,5,7,8-hexaoxonanes (peroxide trimers).

作者信息

Dong Yuxiang, Creek Darren, Chollet Jacques, Matile Hugues, Charman Susan A, Wittlin Sergio, Wood James K, Vennerstrom Jonathan L

机构信息

College of Pharmacy, University of Nebraska Medical Center, 986025 Nebraska Medical Center, Omaha, NE 68198-6025, USA.

出版信息

Antimicrob Agents Chemother. 2007 Aug;51(8):3033-5. doi: 10.1128/AAC.00264-07. Epub 2007 May 7.

DOI:10.1128/AAC.00264-07
PMID:17485500
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1932524/
Abstract

Six tetraoxanes had 50% inhibitory concentrations in the range of 10 to 100 ng/ml against Plasmodium falciparum, whereas the corresponding hexaoxonanes had minimal antimalarial activity. The lack of iron-mediated reactivity of the hexaoxonanes may explain their low activity compared to the tetraoxanes, the latter of which are able to undergo iron(II)-mediated activation.

摘要

六种四氧杂环烷对恶性疟原虫的50%抑制浓度在10至100纳克/毫升范围内,而相应的六氧杂环烷抗疟活性极小。与四氧杂环烷相比,六氧杂环烷缺乏铁介导的反应性可能解释了它们的低活性,四氧杂环烷能够经历铁(II)介导的活化。

相似文献

1
Comparative antimalarial activities of six pairs of 1,2,4,5-tetraoxanes (peroxide dimers) and 1,2,4,5,7,8-hexaoxonanes (peroxide trimers).六对1,2,4,5-四氧杂环己烷(过氧化物二聚体)和1,2,4,5,7,8-六氧杂环辛烷(过氧化物三聚体)的抗疟活性比较
Antimicrob Agents Chemother. 2007 Aug;51(8):3033-5. doi: 10.1128/AAC.00264-07. Epub 2007 May 7.
2
Comparison of the reactivity of antimalarial 1,2,4,5-tetraoxanes with 1,2,4-trioxolanes in the presence of ferrous iron salts, heme, and ferrous iron salts/phosphatidylcholine.抗疟 1,2,4,5-四噁烷与 1,2,4-三噁烷在亚铁盐、血红素和亚铁盐/磷脂存在下的反应性比较。
J Med Chem. 2011 Oct 13;54(19):6443-55. doi: 10.1021/jm200768h. Epub 2011 Sep 19.
3
Synthesis and antimalarial activity of dihydroperoxides and tetraoxanes conjugated with bis(benzyl)acetone derivatives.二氢过氧化物和四氧烷与双(苄基)丙酮衍生物的共轭物的合成及抗疟活性。
Chem Biol Drug Des. 2012 May;79(5):790-7. doi: 10.1111/j.1747-0285.2012.01345.x. Epub 2012 Mar 16.
4
Two-step synthesis of achiral dispiro-1,2,4,5-tetraoxanes with outstanding antimalarial activity, low toxicity, and high-stability profiles.具有出色抗疟活性、低毒性和高稳定性的非手性双螺环-1,2,4,5-四氧杂环己烷的两步合成法。
J Med Chem. 2008 Apr 10;51(7):2170-7. doi: 10.1021/jm701435h. Epub 2008 Mar 15.
5
Tetraoxanes as antimalarials: harnessing the endoperoxide.四氧杂环烷类化合物作为抗疟药物:利用内过氧化物。
Mini Rev Med Chem. 2014 Feb;14(2):123-35. doi: 10.2174/1389557514666140123144942.
6
Chemical stability of the peroxide bond enables diversified synthesis of potent tetraoxane antimalarials.过氧化物键的化学稳定性使得强效四氧烷抗疟药能够进行多样化合成。
J Med Chem. 2008 Apr 10;51(7):2261-6. doi: 10.1021/jm701417a. Epub 2008 Mar 11.
7
Dispiro-1,2,4,5-tetraoxanes: a new class of antimalarial peroxides.双螺-1,2,4,5-四氧杂环己烷:一类新型抗疟过氧化物。
J Med Chem. 1992 Aug 7;35(16):3023-7. doi: 10.1021/jm00094a015.
8
Tetraoxanes: synthetic and medicinal chemistry perspective.四氧杂环丁烷:合成与药物化学视角
Med Res Rev. 2012 May;32(3):581-610.
9
Synthesis, antimalarial activity and cytotoxicity of substituted 3,6-diphenyl-[1,2,4,5]tetraoxanes.取代的3,6-二苯基-[1,2,4,5]四恶烷的合成、抗疟活性及细胞毒性
Bioorg Med Chem. 2009 Aug 1;17(15):5632-8. doi: 10.1016/j.bmc.2009.06.020. Epub 2009 Jun 16.
10
Synthesis, thermal stability, antimalarial activity of symmetrically and asymmetrically substituted tetraoxanes.对称和不对称取代四氧杂环乙烷的合成、热稳定性及抗疟活性
Bioorg Med Chem Lett. 2008 Feb 15;18(4):1446-9. doi: 10.1016/j.bmcl.2007.12.069. Epub 2008 Jan 1.

引用本文的文献

1
Endoperoxide antimalarials: development, structural diversity and pharmacodynamic aspects with reference to 1,2,4-trioxane-based structural scaffold.内过氧化物抗疟药:基于1,2,4-三恶烷结构支架的开发、结构多样性及药效学方面
Drug Des Devel Ther. 2016 Nov 1;10:3575-3590. doi: 10.2147/DDDT.S118116. eCollection 2016.

本文引用的文献

1
Iron-mediated degradation kinetics of substituted dispiro-1,2,4-trioxolane antimalarials.铁介导的取代二螺-1,2,4-三氧杂环戊烷抗疟药的降解动力学
J Pharm Sci. 2007 Nov;96(11):2945-56. doi: 10.1002/jps.20958.
2
Design and synthesis of orally active dispiro 1,2,4,5-tetraoxanes; synthetic antimalarials with superior activity to artemisinin.
Org Biomol Chem. 2006 Dec 21;4(24):4431-6. doi: 10.1039/b613565j. Epub 2006 Nov 3.
3
Synthesis of 1,2,4-trioxepanes via application of thiol-olefin co-oxygenation methodology.通过硫醇-烯烃共氧化方法合成1,2,4-三氧杂环庚烷。
Bioorg Med Chem Lett. 2006 Dec 1;16(23):6124-30. doi: 10.1016/j.bmcl.2006.08.098. Epub 2006 Sep 15.
4
Synthesis and antimalarial activities of novel 3,3,6,6-tetraalkyl-1,2,4,5-tetraoxanes.新型3,3,6,6-四烷基-1,2,4,5-四氧杂环己烷的合成及其抗疟活性
Bioorg Med Chem. 2006 Dec 1;14(23):7790-5. doi: 10.1016/j.bmc.2006.07.069. Epub 2006 Aug 17.
5
Kinetics of iron-mediated artemisinin degradation: effect of solvent composition and iron salt.铁介导的青蒿素降解动力学:溶剂组成和铁盐的影响
J Pharm Sci. 2005 Aug;94(8):1820-9. doi: 10.1002/jps.20400.
6
Dispiro-1,2,4-trioxane analogues of a prototype dispiro-1,2,4-trioxolane: mechanistic comparators for artemisinin in the context of reaction pathways with iron(II).原型双螺-1,2,4-三氧戊环的双螺-1,2,4-三恶烷类似物:在与亚铁反应途径背景下作为青蒿素的机理对照物。
J Org Chem. 2005 Jun 24;70(13):5103-10. doi: 10.1021/jo050385+.
7
Synthetic peroxides as antimalarials.
Curr Opin Investig Drugs. 2004 Aug;5(8):866-72.
8
Synthetic peroxides as antimalarials.作为抗疟药物的合成过氧化物。
Med Res Rev. 2004 Jul;24(4):425-48. doi: 10.1002/med.10066.
9
A medicinal chemistry perspective on artemisinin and related endoperoxides.从药物化学角度看青蒿素及相关内过氧化物。
J Med Chem. 2004 Jun 3;47(12):2945-64. doi: 10.1021/jm030571c.
10
Artemisinin: mechanisms of action, resistance and toxicity.青蒿素:作用机制、耐药性及毒性
Int J Parasitol. 2002 Dec 4;32(13):1655-60. doi: 10.1016/s0020-7519(02)00194-7.