SYNTHESIS OF NOVEL BIOLOGICALLY ACTIVE NATURAL PRODUCTS

新型生物活性天然产物的合成

• 批准号: 3278043
• 负责人: ROBERT K BOECKMAN
• 金额: $ 8.2万
• 依托单位: UNIVERSITY OF ROCHESTER
• 依托单位国家: 美国
• 财政年份: 1982
• 资助国家: 美国
• 起止时间: 1982-09-15 至 1990-08-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/3278043
• 关键词: chemical structure function; cycloalkene; drug design /synthesis /production; sesquiterpenes

The objectives are to develop general protocols for the synthesis of three different classes of naturally occurring compounds, Eremantholide A, Saudin, and Ginkgolide A, each of which possesses interesting biological activity and which constitute a lead in a different therapeutic area, namely cancer, diabetes, and cardiovascular disease, asthma and stroke, respectively. The syntheses have been planned with the idea that simpler analog structures will become available during our studies to assist in the development of structure activity relationships in these unique classes of compounds. Our studies will explore new strategies and new applications and methods for creation of contiguous quaternary centers, closure of medium rings, and the construction of hetero propellane systems. The problems posed by these densely functionalized cage and bridged ring structures present considerable challenges for contemporary synthetic organic chemistry.

目标是开发合成三种化合物的通用方案 不同类别的天然化合物，Eremantholide A， 沙丁 (Saudin) 和银杏内酯 A (Ginkgolide A) 均具有有趣的生物活性 活动并构成不同治疗领域的领先地位， 即癌症、糖尿病、心血管疾病、哮喘和中风， 分别。 合成的设计理念是更简单的模拟 在我们的研究期间将提供结构来协助 这些独特类别中结构活动关系的发展 化合物。 我们的研究将探索新的策略和新的应用和方法 用于创建连续的四元中心、闭合中环，以及 异质推进系统的构建。 这些带来的问题 存在密集功能化的笼形结构和桥环结构 当代合成有机化学面临着巨大的挑战。