...
  • 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Synthesis of stavudine amino acid ester prodrugs with broad-spectrum chemotherapeutic properties for the effective treatment of HIV/AIDS.
【24h】

Synthesis of stavudine amino acid ester prodrugs with broad-spectrum chemotherapeutic properties for the effective treatment of HIV/AIDS.

机译：具有广谱化学治疗特性的司他夫定氨基酸酯前药的合成，可有效治疗HIV / AIDS。

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

A series of prodrugs of stavudine were synthesized in an effort to enhance spectrum of chemotherapeutic properties for the effective treatment of HIV/AIDS. The 5'-OH function of stavudine was esterified with ciprofloxacin, norfloxacin, isoniazide, pyrazinamide, piperazine and dimethylamine acetic acid. The anti-HIV-1 activity of the esters was determined in CEM cell line and stavudine ester bearing piperazine acetic acid was found to be the most potent compound with a selective index of >15,723. Stavudine prodrug bearing ciprofloxacin and norfloxacin acetic acid showed 100% inhibition against Mycobacterium tuberculosis H(37)Rv at 6.25 microg/mL. The prodrugs also exhibited antibacterial activity against 24 pathogenic bacteria. In vitro hydrolysis of the various esters in human plasma indicated that these agents were relatively stable toward plasma esterases with t(1/2) ranging from 20-240 min.
机译：为了增强有效治疗HIV / AIDS的化学治疗谱，合成了司他夫定的一系列前药。将司他夫定的5'-OH功能用环丙沙星，诺氟沙星，异烟肼，吡嗪酰胺，哌嗪和二甲胺乙酸酯化。在CEM细胞系中测定了这些酯的抗HIV-1活性，发现带有司他夫定酯的哌嗪乙酸是最有效的化合物，选择性指数> 15,723。带有环丙沙星和诺氟沙星乙酸的斯达夫定前药在6.25 microg / mL下对结核分枝杆菌H（37）Rv表现出100％的抑制作用。前药还表现出对24种病原菌的抗菌活性。人血浆中各种酯的体外水解表明，这些试剂对血浆酯酶相对稳定，t（1/2）范围为20-240分钟。

著录项

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