IRON TRANSPORT MEDIATED DRUG DELIVERY SYSTEMS - SYNTHESIS AND ANTIBACTERIAL ACTIVITY OF SPERMIDINE-BASED AND LYSINE-BASED SIDEROPHORE-BETA-LACTAM CONJUGATES

被引:37
作者
MCKEE, JA [1 ]
SHARMA, SK [1 ]
MILLER, MJ [1 ]
机构
[1] UNIV NOTRE DAME,DEPT CHEM & BIOCHEM,NOTRE DAME,IN 46556
关键词
D O I
10.1021/bc00010a013
中图分类号
Q5 [生物化学];
学科分类号
071010 ; 081704 ;
摘要
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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页码:281 / 291
页数:11
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