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对增强抗菌活性的非规范性,动态共价单环和多环宏循环的多功能方法
James F Reuther1, Andrew C Goodrich2, P Rogelio Escamilla1
1Department of Chemistry , University of Texas at Austin , Austin , Texas 78712 , United States.
Journal of the American Chemical Society
|February 22, 2018
概括
研究人员开发了一种用于增强抗菌剂的复杂宏循环 (MC) 的新方法. 这种技术通过形成单环,双环和三环来提高现有的抗菌的有效性.
科学领域:
- 生物化学
- 医学化学
- 材料科学
背景情况:
- 由于其生物相容性和可调性,类寡合物是抗菌剂的有希望的支架.
- 形成具有多个循环的复杂宏循环 (MCs) 是治疗开发中的一个重大挑战.
研究的目的:
- 开发一种用于创建单环,双环和三环宏循环 (MC) 的多功能方法.
- 使用这些新型宏循环结构来增强的抗菌性质.
主要方法:
- 使用二甲或二化交叉连接剂的动态凝.
- 用含有的侧链在水化物C端树脂上合成的,用于树脂组装.
- 使用MALDI-TOF MS,HPLC和SDS-PAGE确认了宏循环的形成.
主要成果:
- 成功形成单环,双环和三环MC.
- 在树脂切割时直接实现可调节的MC组件.
- 当被纳入宏循环结构时,证明了布福林II抗菌性能的显著增强.
结论:
- 动态共价化学为构建复杂宏循环提供了一种多功能方法.
- 与线性序列相比,通过水凝结的宏环化显著提高了抗菌疗效.
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