SYNTHETIC STUDIES ON COMPLEX NATURAL PRODUCTS

复杂天然产品的综合研究

• 批准号: 3394717
• 负责人: YOSHITO KISHI
• 金额: $ 43.53万
• 依托单位: HARVARD UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 1978
• 资助国家: 美国
• 起止时间: 1978-06-01 至 1995-05-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/3394717
• 关键词: alkaloids; antibiotics; beta glucosidases; blood group antigens; calcium binding protein; calcium metabolism; chemical structure function; conformation; drug design /synthesis /production; drug metabolism; ionophores; maltose; neurophysiology; neurotoxins; oligopeptides; oligosaccharides; organic chemicals; saxitoxin; stereoisomer; sucrose

The major objective in this research is to make significant contributions to organic chemistry and medicine through synthetic studies on physiologically active natural and man-made organic compounds, including 1. the total synthesis and conformational analysis of the marine natural product palytoxin, 2. the synthesis and conformational analysis of oligosaccharides and their carbon analogues such as cellobiose, maltose, human blood group antigens, and sucrose, 3. the synthesis and conformational analysis of semi-synthetic polyether antibiotics, 4. the development of organic solvent soluble 310-helical oligopeptides, 5. semi- synthetic aequorins as a tool of the determination of local calcium concentration on the intact cells, and 6. enantioselective synthesis of saxitoxins and gonyautoxins. We believe that the power of organic chemistry is most effectively extended by challenging complex systems, and much of the progress of medicine critically depends upon the extension of the power of organic chemistry. It is also our specific objective to develop practical and efficient syntheses of certain natural products and their analogues which have high physiological activity, but are not available in appreciable amount from natural sources. These studies are again expected to stimulate the progress in medicine.

本研究的主要目标是取得重大成果 通过合成对有机化学和医学的贡献 具有生理活性的天然和人造有机物的研究 化合物，包括1.全合成和构象 海洋天然产物海藻毒素的分析、2.合成 寡糖及其碳的构象分析 纤维二糖、麦芽糖、人类血型等类似物 抗原、蔗糖，3.合成与构象分析 4.半合成聚醚类抗生素的开发 有机溶剂可溶的310螺旋寡肽，5.半 合成水母发光蛋白作为测定局部的工具 完整细胞上的钙浓度，以及 6. 对映选择性 石房蛤毒素和膝沟藻毒素的合成。 我们相信 有机化学的力量最有效地扩展是 挑战复杂的系统，以及许多进展 医学关键取决于力量的扩展 有机化学。 开发实用、高效的产品也是我们的具体目标 某些天然产物及其类似物的合成 具有较高的生理活性，但不存在于 相当数量的天然来源。 这些研究再次 有望推动医学进步。