SYNTHESIS OF HIGH MOLECULAR WEIGHT IRON CHELATORS

IN CHEMICAL AND BIOLOGICAL SYSTEMS, IRON IS BOTH UBIQUITOUS AND HIGHLY REACTIVE. IN A VARIETY OF CIRCUMSTANCES, THERE IS GREAT NEED FOR NEW APPROACHES TO THE REMOVAL OF IRON OR THE CONTROL OF ITS REACTIVITY. BIOMEDICAL FRONTIERS HAS PRODUCED A SERIES OF HIGH MOLECULAR WEIGHT IRON CHELATORS BASED ON DERIVATION OF A NUMBER OF SUBSTRATES WITH DEFER- OXAMINE B. THIS CHELATOR HAS AN EXTREMELY HIGH AFFINITY FORIRON AND IS VERY SELECTIVE (I.E., HAS RELATIVELY LOW AFFINITY FOR OTHER POLYVALENT CATIONS ASIDE FROM ALUMINUM). ADDUCTS HAVE BEEN PRODUCED BETWEEN DEFEROXAMINE B AND BOTH SOLUBLE POLYMERS AND SOLID MATRICES. THE PRESENT PROPOSAL RELATES TO MAXIMIZATION OF DERIVATION PROCEDURES, DEFINITIONOF APPROPRIATE CONDITIONS OF MODIFICATION, AND DETERMINATIONOF THE PHYSICAL CHARACTERISTICS OF THE DERIVED MATERIALS. THE HIGH MOLECULAR WEIGHT IRON CHELATORS PRODUCED AS A RESULT OF THIS WORK HAVE A NUMBER OF POTENTIAL (PHASE II) APPLICATIONS. THESE INCLUDE: (1) THE SELECTIVE AND QUANTITATIVE REMOVAL OF IRON FROM SOLUTIONS, (2) A SIMPLE AND RAPID PROCEDURE FOR SERUM IRON DETERMINATION, (3) MORE EFFECTIVE IRON CHELATION THERAPY, AND (4) THE CONTROL OF BACTERIAL INFECTIONS THAT ARE PROMOTED BY FREE IRON.