PHYSIOLOGICALLY ACTIVE NATURAL PRODUCTS

生理活性天然产品

• 批准号: 6387044
• 负责人: DOUGLASS F. TABER
• 金额: $ 19.95万
• 依托单位: UNIVERSITY OF DELAWARE
• 依托单位国家: 美国
• 财政年份: 2000
• 资助国家: 美国
• 起止时间: 2000-04-01 至 2004-03-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6387044
• 关键词: alkaloids; biological products; carbene; carbopolycyclic compound; cyclization; diterpenes; drug design /synthesis /production; morphine

Both the recent resurgence of infectious disease and the abiding interest in new tools for neuropharmacology have driven the continuing effort to isolate and establish the structures of new active agents from natural sources. While some of these might well be useful leads for pharmaceutical development, often the structurally more complex agents will not be pursued, because of perceived difficulties with their synthesis. An investigation of a new method for the construction of carbocyclic rings, intramolecular alkylidene C-H insertion, is proposed. This already shows the promise of becoming a powerful tool for target-directed synthesis. Specific targets include the cognition-enhancing alkaloid huperzine A, morphine, the parent compound of the morphine alkaloids, and N-deacetyllappaconitine, representative of the Delphinium diterpenoid alkaloids.

最近传染病的死灰复燃以及对神经药理学新工具的持续兴趣推动了从天然来源中分离和建立新活性剂结构的持续努力。 虽然其中一些很可能是药物开发的有用线索，但结构上更复杂的药物通常不会被采用，因为它们的合成存在困难。 提出了一种构建碳环的新方法——分子内亚烷基C-H插入的研究。 这已经显示出成为目标导向合成的强大工具的希望。 具体目标包括增强认知的生物碱石杉碱甲、吗啡（吗啡生物碱的母体化合物）和 N-脱乙酰高乌甲碱（飞燕草二萜生物碱的代表）。