揭开拉帕米辛小调整剂的真实身份
Emily B Crull1, Ajay N Jain2, Paul C D Hawkins3
1Department of Chemistry and Biochemistry, University of North Carolina Wilmington, Wilmington, North Carolina 28409, United States.
Journal of natural products
|July 11, 2023
概括
拉巴胺的小溶液构成者是胺转化物,而不是之前假设的cis. 这一发现,通过NMR和计算方法确定,澄清了拉帕素.
科学领域:
- 自然产品 化学 化学
- 结构生物学 结构生物学
- 有机化学 有机化学
背景情况:
- 拉帕米是一种天然产品,表现出多种生物活性.
- 拉帕米辛存在于溶液中的两种构成的混合物中.
- 小溶液符合的结构以前没有表征,通过类比假定cis amide.
研究的目的:
- 为了确定拉帕素小形态的溶液结构.
- 解决关于小调整器的 cis/trans amide 配置的长期问题.
主要方法:
- 核磁共振 (NMR) 光谱学.核磁共振 (NMR) 光谱学.
- 计算建模技术. 计算建模技术.
- 溶液状态结构动态的分析.
主要成果:
- 溶液中拉帕米的小构造者是一种转胺物种.
- 围绕埃斯特连接的旋转有助于小适配体的结构.
- 之前假设的cis amide配置被证明是不成立的.
结论:
- 拉帕米的小调整剂的溶液结构被确定为特兰斯胺.
- 这一发现纠正了基于结构类比的长期假设.
- 澄清了溶液中拉帕米的构造格局.
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