Conceptually, the penetration of beta-lactam antibiotics through the bacterial cell wall can be enhanced by utilizing various active transport systems such as the active iron-transport system that exists in bacteria. Several beta-lactam-siderophore analogue (microbial iron chelators) conjugates were prepared to investigate this approach. Thus, monocyclic (oxamazin) and bicyclic (carbacephalosporin) beta-lactams were separately linked to dihydroxybenzoyl derivatives of spermidine and lysine. The antibacterial activity of these conjugates has been investigated and the potential use of the iron-transport system as a drug-delivery system is discussed.
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McKee et al. (1991) studied this question.
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