斯特拉塞里奥利德A和斯特拉塞里奥利德B的总合成,它们是强大的抗疟疾药物
Arun K Ghosh1, John P Gulliver1
1Department of Chemistry, Department of Medicinal Chemistry and Molecular Pharmacology, Purdue University, 560 Oval Drive, West Lafayette, Indiana 47907, United States.
The Journal of organic chemistry
|August 9, 2024
概括
研究人员合成了斯特拉塞里奥利德A和B,这是来自新西兰植物的强有力的抗疟疾化合物. 这些分子对疟疾寄生虫Plasmodium falciparum表现出显著的活动.
科学领域:
- 有机化学 有机化学
- 药用化学 医学化学
- 自然产品 化学 化学
背景情况:
- 斯特拉塞里奥利德A和B是最近发现的具有强大的抗疟疾活性的天然产品.
- 这些化合物是从新西兰原产的一种未知的植物物种中分离出来的.
研究的目的:
- 为了实现第一个聚变的斯特拉塞里奥利德A和B的总合成.
- 确认这些抗疟剂的结构并探索这些抗疟剂的化学空间.
主要方法:
- 合成采用了不对称的syn-aldol,不对称的化和不对称的约翰逊-克莱森重排,以建立立体中心.
- 关键步骤包括山口巨乳形成的巨乳形成,格拉布斯的交叉转移和NHK合.
主要成果:
- 成功执行了斯特拉塞里奥利德A和B的融合总合成.
- 斯特拉塞里奥利德A的合成涉及27个总步骤和16个最长的线性步骤.
- 通过立体选择性反应在斯特拉塞里奥利德B中建立了七个性中心中的六个.
结论:
- 总合成可以获得有价值的抗疟疾化合物.
- 开发的合成策略可以应用于相关的天然产品或类似产品.
相关概念视频
Combined Effects of Drugs: Synergism
3.8K
Synergism is a useful mechanism where combining two or more drugs is more effective than each constituent used alone. Such combinations are also called supra-additive interactions. The drugs collectively enhance the final therapeutic effect by acting on different targets. Another advantage is that the low dose of each constituent drug is sufficient to achieve the desired effect. This helps reduce the duration of therapy and lower the adverse effects of these drugs.
Such synergistic combinations...
Such synergistic combinations...
3.8K
Aryldiazonium Salts to Azo Dyes: Diazo Coupling
2.9K
The reaction of weakly electrophilic aryldiazonium (also called arenediazonium) salts with highly activated aromatic compounds leads to the formation of products with an —N=N— link, called an azo linkage. This reaction, presented in Figure 1, is known as diazo coupling and occurs without the loss of the nitrogen atoms of the aryldiazonium salt. Highly activated aromatic compounds such as phenols or arylamines favor the diazo coupling reaction. The coupling generally occurs at the...
2.9K
![Cercosporin-Photocatalyzed [4+1]- and [4+2]-Annulations of Azoalkenes Under Mild Conditions](/_next/image?url=https%3A%2F%2Fcloudfront.jove.com%2FCDNSource%2Fteasers%2F60786.jpg&w=3840&q=50)

