| 摘要 |
The invention relates to novel conjugates of beta-lactam antibiotics of the general formula (I) with tetra- or hexadentate iron chelators or the acylated derivatives thereof as siderophore components, derived from amino acids or peptides, comprising at least 2 catechol substituents. In formula (I), R<1> represents a beta-lactam antibiotic, optionally with an intercalated further amino acid moiety, or R<1> represents various groups that contain a catechol or hydroxamate group as a complement to a hexadentate chelator structure, optionally in the acylated form or together with spacer groups, and that further contain the group of a beta-lactam antibiotic, especially of a penicillin or cephalosporin derivative, especially ampicillin, amoxicillin or cefaclor (as a free acid, in the form of their salts or their easily cleavable esters). The inventive compounds can be introduced into bacterial cells via the iron transport pathways on account of their siderophore components, thereby efficiently improving or enlarging their activity to a greater extent than known compounds of the kind. The inventive compounds are capable of overcoming resistances of problematic germs that cannot be treated.
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