含异环的合成,反应,功能化和ADMET特性
Scott J Barraza1, Scott E Denmark1
1Roger Adams Laboratory, Department of Chemistry , University of Illinois , Urbana , Illinois 61801 , United States.
Journal of the American Chemical Society
|May 16, 2018
概括
在药物设计方面具有独特的优势, 新的方法可以合成各种含的药物候选物进行生物评估.
科学领域:
- 医学化学
- 药物发现
- 有机化学
背景情况:
- 由于有机化合物的合成方法有限,在药物设计中的潜力未得到充分利用.
- 的独特特性可以提高药物效能和物理化学/ADMET特征.
研究的目的:
- 开发用于将纳入候选药物的新型合成策略.
- 为药物发现创建多种含异循环.
- 评估含化合物的生物特性.
主要方法:
- 为含有的四化和四化构建块开发灵活的多克尺度合成.
- 适应常见反应以快速构建功能化含异环.
- 对精选的化合物及其碳类似物进行以ADMET为重点的比较生物学研究.
主要成果:
- 成功合成含的新型构件和异环.
- 证明了新方法对有机药物支架的快速多样化的有用性.
- 提供对ADMET特性影响的初始生物数据.
结论:
- 一个新的构件策略促进了各种含有的候选药物的合成.
- 有机化合物有望改善药物特性,需要进一步研究.
- 这项工作解决了一个关键的合成缺口,为在药物设计中的更广泛使用铺平了道路.
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