MULTIDENTATE TEREPHTHALAMIDATE AND HYDROXYPYRIDONATE LIGANDS [electronic resource] : TOWARDS NEW ORALLY ACTIVE CHELATORS

• Ngôn ngữ: eng
• Ký hiệu phân loại: 546.7 Groups 15, 16, 17, 18
• Thông tin xuất bản: Berkeley, Calif. : Oak Ridge, Tenn. : Lawrence Berkeley National Laboratory ; Distributed by the Office of Scientific and Technical Information, U.S. Dept. of Energy, 2011
• Mô tả vật lý: Size: 276 : , digital, PDF file.
• Bộ sưu tập: Metadata
• ID: 262339
• Chủ đề: 1. 37 inorganic, organic, physical and analytical chemistry; 2. 38 radiation chemistry, radiochemistry, and nuclear chemistry; 3. 59 basic biological sciences; 4. 60 applied life sciences; 5. Actinides; 6. Affinity; 7. Chelating agents; 8. Contamination; 9. Deferoxamine; 10. Dtpa; 11. Et al

Tóm tắt

The limitations of current therapies for the treatment of iron overload or radioisotope contamination have stimulated efforts to develop new orally bioavailable iron and actinide chelators. Siderophore-inspired tetradentate, hexadentate and octadentate terephthalamidate and hydroxypyridonate ligands were evaluated in vivo as selective and efficacious iron or actinide chelating agents, with several metal loading and ligand assessment procedures, using {sup 59}Fe, {sup 238}Pu, and {sup 241}Am as radioactive tracers. The compounds presented in this study were compared to commercially available therapeutic sequestering agents [deferoxamine (DFO) for iron and diethylenetriaminepentaacetic acid (DPTA) for actinides] and are unrivaled in terms of affinity, selectivity and decorporation efficacy, which attests to the fact that high metal affinity may overcome the low bioavailability properties commonly associated to multidenticity.