Iron transport mediated drug delivery systems: synthesis and antibacterial activity of spermidine- and lysine-based siderophore - .beta.-lactam conjugates
- 1 July 1991
- journal article
- research article
- Published by American Chemical Society (ACS) in Bioconjugate Chemistry
- Vol. 2 (4) , 281-291
- https://doi.org/10.1021/bc00010a013
Abstract
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.Keywords
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