• 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum
【24h】

Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum

机译：芳香族双氨基氨基氨基铵对疟原虫的合成，生物学特征及结构活性关系

获取原文
获取原文并翻译 | 示例
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

Malaria is one of the most significant tropical diseases and remains a major challenge due to the lack of a broadly effective vaccine and parasite resistance to current drugs. This means there is a need for new drug candidates with novel modes of action. Aromatic bisamidines, such as furamidine (DB75), were initially developed as anti-Trypanosoma agents however as clinical trials with furamidine highlighted potential side effects they were not pursued further in that setting. Despite apparent cytotoxicity liabilities the potency of furamidine against Plasmodium falciparum makes it a promising scaffold for the development of new anti-Plasmodium agents with improved selectivity. In this study a bisamidine compound series based on furamidine was synthesized by introducing modifications at the furan core structure and terminal amidine groups. The activity of the derived compounds was tested in vitro against drug sensitive and resistant P. falciparum lines and a human cell line (HEK293 cells) to generate anti Plasmodium structure-activity relationships and to provide preliminary selectivity data. (C) 2016 Elsevier Masson SAS. All rights reserved.
机译：疟疾是最重要的热带疾病之一，仍然是由于缺乏广泛有效的疫苗和寄生虫对目前药物的主要挑战。这意味着需要具有新的新药候选者具有新的动作模式。芳香bisamidines，如furamidine（DB75），最初被开发为抗锥虫药然而与furamidine临床试验中强调潜在的副作用，他们没有进一步在该环境中追求的。尽管表现明显的细胞毒性负债，但Furamidine对疟原虫的效力使Falciparum的效力使其成为开发新的抗疟原虫剂，具有改善的选择性的有前途的脚手架。在本研究中，通过在呋喃核心结构和脒基团的末端进行改性，合成基于呋喃尼的双酰胺化合物系列。在体外测试衍生化合物的活性抵抗药物敏感和抗性的抗性疟原虫线和人细胞系（HEK293细胞），以产生抗疟原虫结构 - 活性关系，并提供初步选择性数据。 （c）2016年Elsevier Masson SAS。版权所有。

著录项

  • 来源
  • 作者

    Sauer B.; Skinner-Adams T. S.; Bouchut A.; Chua M. J.; Pierrot C.; Erdmann F.; Robaa D.; Schmidt M.; Khalife J.; Andrews K. T.; Sippl W.;

  • 作者单位

    Martin Luther Univ Halle Wittenberg Wolfgang Langenbeck Str 4 D-06120 Halle Germany;

    Griffith Univ Trop Parasitol Lab Eskitis Inst Drug Discovery Don Young Rd Nathan Qld 4111;

    Univ Lille Nord France Inst Pasteur Lille CNRS UMR 8204 U1019 1 Rue Prof Calmette F-59019 Lille;

    Griffith Univ Trop Parasitol Lab Eskitis Inst Drug Discovery Don Young Rd Nathan Qld 4111;

    Univ Lille Nord France Inst Pasteur Lille CNRS UMR 8204 U1019 1 Rue Prof Calmette F-59019 Lille;

    Martin Luther Univ Halle Wittenberg Wolfgang Langenbeck Str 4 D-06120 Halle Germany;

    Martin Luther Univ Halle Wittenberg Wolfgang Langenbeck Str 4 D-06120 Halle Germany;

    Martin Luther Univ Halle Wittenberg Wolfgang Langenbeck Str 4 D-06120 Halle Germany;

    Univ Lille Nord France Inst Pasteur Lille CNRS UMR 8204 U1019 1 Rue Prof Calmette F-59019 Lille;

    Griffith Univ Trop Parasitol Lab Eskitis Inst Drug Discovery Don Young Rd Nathan Qld 4111;

    Martin Luther Univ Halle Wittenberg Wolfgang Langenbeck Str 4 D-06120 Halle Germany;

  • 收录信息
  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 药学;
  • 关键词

    Plasmodium falciparum; Bisamidine; Furamidine; Cytotoxicity;

    机译：疟原虫疟原虫;二氨基;呋喃尼;细胞毒性;

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号