| abstract |
The invention relates to new derivatives of benzoxazinedione and to their covalent compounds with active ingredients, in particular antibiotics. The compounds are heterocyclic protected catechol compounds and are effective as siderophores against strains of gram-negative bacteria, especially against pseudomonads and E. coli and Salmonella strains. In the form of covalent compounds with active ingredients, in particular antibiotics (in the form of "siderophore-antibiotic compounds"), they can transfer to the bacterial cell active ingredients through the transport of iron and therefore can increase their antibacterial efficiency and expand the scope, sometimes even in relation to strains of bacteria resistant to other -lactams. In addition, these compounds, as potential prodrugs for iron chelating agents, are useful in the treatment of diseases caused by disorders of iron metabolism. The invention can be used in pharmaceutical research and in the pharmaceutical industry, as well as in agriculture. Formula I: where R1 = Η or carboxyalkyl, R2 = H, alkyl or phenyl, and R3 represents various acid groups derived from amino acids, dipeptides and hydrazones or their covalent compounds with active ingredients, in particular antibiotics. These compounds may exist in the form of free acids, in the form of their salts or in the form of an ester which is easily cleaved. |