title: Bis(3-hydroxy-4-pyridinone)-EDTA derivative as a potential therapeutic Al-chelating agent. Synthesis, solution studies and biological assays.
abstract: The 3-hydroxy-4-pyridinones are chelating agents of current interest due to their high affinity for hard metal ions and potential clinical applications as metal-decorporation agents. A new bis-(3-hydroxy-4-pyridinone) derivative of EDTA have been developed, and herein we describe the results of solution studies to determine the protonation constants and the partition coefficient. Biodistribution studies, performed with 67Ga-overload mice, showed rapid clearance of the radiotracer from the body, thus indicating that the new ligand should be a quite effective agent for the in vivo aluminium removal.
authors.affiliation: Centro de Química Estrutural, Complexo I, Instituto Superior Técnico, Av. Rovisco Pais, 1, 1049-001 Lisboa, Portugal. masantos@ist.utl.pt
authors.forename: M Amélia
authors.initials: MA
authors.lastname: Santos
authors.forename: Sofia
authors.initials: S
authors.lastname: Gama
authors.forename: Lurdes
authors.initials: L
authors.lastname: Gano
authors.forename: Etelka
authors.initials: E
authors.lastname: Farkas
mesh_terms: D000535:Aluminum / Q000737:chemistry*; D000818:Animals; D002614:Chelating Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D004492:Edetic Acid / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D005260:Female; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D012996:Solutions; D014018:Tissue Distribution
chemical_list: D002614:Chelating Agents; D012996:Solutions; C506756:ethylenodiamino-N,N'-bis(acetocarboxyl)-N,N'-bis(acetyl(1-(3'-aminopropyl)-3-hydroxy-2-methyl-4-pyridinone)); D004492:Edetic Acid; D000535:Aluminum