IRON TRANSPORT-MEDIATED DRUG-DELIVERY - SYNTHESIS AND BIOLOGICAL EVALUATION OF CYANURIC ACID-BASED SIDEROPHORE ANALOGS AND BETA-LACTAM CONJUGATES

被引：34

作者：

GHOSH, M ^{[1
]}

MILLER, MJ ^{[1
]}

机构：

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

来源：

JOURNAL OF ORGANIC CHEMISTRY | 1994年 / 59卷 / 05期

关键词：

D O I：

10.1021/jo00084a018

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Trihydroxamate-containing isocyanurates 4a-c were synthesized and determined to be capable of substituting for natural siderophores (microbial iron sequestering agents) in limited microbiological assays. The direct coupling of protected 4a to carbacephalosporins 16 and 17 and subsequent deprotection gave conjugates 20 and 21. The Lorabid conjugate 21 was especially active against E. coli X580 in preliminary biological tests, thus demonstrating the continued potential of siderophore-mediated drug delivery.

引用

页码：1020 / 1026

页数：7

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