DESIGN, SYNTHESIS, AND BIOLOGICAL EVALUATION OF ISOCYANURATE-BASED ANTIFUNGAL AND MACROLIDE ANTIBIOTIC CONJUGATES - IRON TRANSPORT-MEDIATED DRUG-DELIVERY

被引：30

作者：

GHOSH, M ^{[1
]}

MILLER, MJ ^{[1
]}

机构：

[1] UNIV NOTRE DAME, DEPT CHEM & BIOCHEM, NOTRE DAME, IN 46556 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 1995年 / 3卷 / 11期

关键词：

D O I：

10.1016/0968-0896(95)00134-3

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The syntheses and preliminary biological evaluation of conjugates of a synthetic isocyanurate-based trihydroxamate siderophore with two antifungal agents, 5-FU (conjugate 9) and norneoenactin (conjugate 12), and a macrolide antibiotic, erythromycylamine (conjugate 18), are described. A F-19 NMR study was used to determine the hydrolytic stability of conjugate 9 under assay conditions. Preliminary biological studies with ferric complexes of conjugates 9 and 12 indicated that these antifungal agents are recognized by Candida and perhaps are actively transported into the cell by the siderophore-transport mechanisms. While conjugate 18 did not show any significant antibacterial activity, presumably due to size restriction, the 5-FU conjugate 9 appeared to be moderately active against a variety of Gram-positive strains, and was more active than the 5-FC control against some strains of Staphylococcus

引用

页码：1519 / 1525

页数：7

共 33 条

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