...
  • 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Journal of Medicinal Chemistry >Dissecting the Structure of Thiopeptides: Assessment of Thiazoline and Tail Moieties of Baringolin and Antibacterial Activity Optimization
【24h】

Dissecting the Structure of Thiopeptides: Assessment of Thiazoline and Tail Moieties of Baringolin and Antibacterial Activity Optimization

机译：解剖硫肽的结构：Baringolin的噻唑啉和尾部的评估和抗菌活性的优化

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

Several analogues of baringolin (1) were prepared to evaluate the role of its characteristic thiazoline ring and pentapeptidic tail with the aim of defining structure? activity relationships for these moieties. The thiazoline ring appeared as a crucial moiety to maintain a broad scope of activities against different Gram-positive bacteria. Further modifications were performed to simplify the structure of the natural product and assess the role of its tail, resulting in an enhanced in vitro performance. Analogue 25, with the thiazolecontaining macrocycle and a 4-aminocyclohexane-1-carboxylic acid moiety in place of the pentapeptidic tail, was identified as a much more potent analogue, capable of overcoming the absence of the thiazoline ring and performing extraordinarily well against all strains tested. This is the first library of thiopeptide analogues produced by chemical synthesis alone, which demonstrates the robustness and convenience of the synthetic strategy used.
机译：准备了几种Baringolin（1）的类似物，以评估其特征性的噻唑啉环和五肽尾巴的作用，以定义结构。这些部分的活动关系。噻唑啉环似乎是维持针对不同革兰氏阳性细菌的广泛活性范围的关键部分。进行了进一步的修饰以简化天然产物的结构并评估其尾巴的作用，从而增强了体外性能。含有噻唑的大环和4-氨基环己烷-1-羧酸部分代替五肽尾巴的类似物25被鉴定为更有效的类似物，能够克服噻唑啉环的缺失并能很好地抵抗所有菌株经过测试。这是单独通过化学合成生产的第一个硫肽类似物文库，证明了所用合成策略的鲁棒性和便利性。

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