McKee J A, Sharma S K, Miller M J
Department of Chemistry and Biochemistry, University of Notre Dame, Indiana 46556.
Bioconjug Chem. 1991 Jul-Aug;2(4):281-91. doi: 10.1021/bc00010a013.
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.
从概念上讲，β-内酰胺类抗生素穿过细菌细胞壁的渗透作用可通过利用各种主动转运系统来增强，比如细菌中存在的主动铁转运系统。制备了几种β-内酰胺-铁载体类似物（微生物铁螯合剂）缀合物来研究这种方法。因此，单环（恶嗪）和双环（碳头孢菌素）β-内酰胺分别与亚精胺和赖氨酸的二羟基苯甲酰衍生物相连。已对这些缀合物的抗菌活性进行了研究，并讨论了铁转运系统作为药物递送系统的潜在用途。
