开发了与DNA相容的S-葡萄糖转换
Qingyi Zhao1,2, Yandan Bao1,2, Dawen Niu3,4
1School of Chinese Materia Medica, Nanjing University of Chinese Medicine, 138 Xianlin Road, Nanjing 210023, China.
Organic letters
|June 26, 2023
概括
我们开发了两种DNA兼容的S-glycosyl转换,用于创建糖基化DNA编码库 (DEL). 使用基糖硫的光诱导方法显示了广泛的兼容性和效率,用于合成新型的甘氨酸DELs.
科学领域:
- 有机化学 有机化学
- 化学生物学 化学生物学
- 药用化学 医学化学
背景情况:
- DNA编码库 (DEL) 是药物发现的强大工具.
- 合成各种DEL的高效方法至关重要.
- 将碳水化合物纳入DEL可以扩大化学空间和治疗潜力.
研究的目的:
- 开发与DNA编码图书馆构建相容的新型S-glycosyl转换.
- 探索将糖与DNA结合分子结合的高效方法.
- 为了创建用于药物发现和输送系统应用的糖基化DEL.
主要方法:
- 研究了2-chloro-1,3-dimethylimidazolidinium chloride (DMC) 介导的S-糖化与未受保护的糖.
- 开发了一种光诱导的,基于激素的S-glycosyl转化,使用基糖硫.
- 在绿光照射下对DNA结合化合物进行结合.
主要成果:
- 以DMC为媒介的方法对DEL构造的基板范围有限.
- 光诱导方法证明了功能组与糖和的良好兼容性.
- 通过光诱导方法实现了与DNA结合的糖衍生物的良好至优良的转化.
结论:
- 光诱导的S-glycosyl转化是一种开创性的,与DNA兼容的合成糖DELs的方法.
- 这种方法为制备各种糖基化化合物提供了有价值的工具.
- 允许探索含糖输送系统和治疗剂的新途径.
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