FERRIC ION SEQUESTERING AGENTS: IRON REMOVAL IN MAN

三价铁离子螯合剂：人体除铁

• 批准号: 3231395
• 负责人: KENNETH N RAYMOND
• 金额: $ 14.7万
• 依托单位: UNIVERSITY OF CALIFORNIA BERKELEY
• 依托单位国家: 美国
• 财政年份: 1983
• 资助国家: 美国
• 起止时间: 1983-11-30 至 1987-11-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/3231395
• 关键词: acylation; blood transfusion; chelating agents; chelation therapy; chemical reaction; chronic disease /disorder; deferoxamine; drug administration rate /duration; drug design /synthesis /production; electrochemistry; heart disorder; iron storage disorder; ligands; liver disorder; orphan disease /drug; pancreas disorder; secretion; sickle cell anemia; thalassemia; thermodynamics; transferrin

A number of polycatechol chelating agents have been prepared using the 2,3-dihydroxybenzoyl (DHB) group or derivatives of it in which the benzoic acid ring has been substituted at the five position by -SO3- or at the four position by -CO2-. In each case the DHB groups are appended to a polyamine backbone. To date, linear triamines (such as spermidine), 1,3,5,-triaminomethylbenzene, and the tripod amine triaminoethylamine have all been used as molecular skeletons. During the next year we intend to continue to explore the synthesis of 4-carboxyl-substituted derivatives of DHB in tricatechol chelating agents. Depending upon the results of animal tests, attempts will be made to optimize the geometries of these complexes through variation of the backbone structure. We also plan to explore new molecular architectures for ferric chelating agents, and examine the thermodynamic properties of those prepared to date.

已经使用本发明制备了许多聚儿茶酚螯合剂。 2，3-二羟基苯甲酰基（DHB）或其衍生物，其中苯甲酸 环在5位被-SO 3-取代或在4位被-SO 3-取代 二氧化碳-。 在每种情况下，DHB基团附加到聚胺主链上。 到 枣、直链三胺（如亚精胺）、1，3，5-三氨基甲基苯，和 三脚架胺三氨基乙胺都被用作分子骨架。 在下一年，我们打算继续探讨综合 三儿茶酚螯合剂中DHB的4-羧基取代衍生物。 根据动物试验的结果，将尝试优化 这些配合物的几何形状通过骨架结构的变化。 我们还计划探索铁螯合剂的新分子结构， 并检查迄今为止制备的那些的热力学性质。