多弹头铁载体-5-氟尿苷缀合物的合成与研究

Syntheses and studies of multiwarhead siderophore-5-fluorouridine conjugates.

作者信息

Lu Y, Miller M J

机构信息

Department of Chemistry and Biochemistry, University of Notre Dame, IN 46556-5670, USA.

出版信息

Bioorg Med Chem. 1999 Dec;7(12):3025-38. doi: 10.1016/s0968-0896(99)00248-5.

DOI:10.1016/s0968-0896(99)00248-5

PMID:10658609

Abstract

Siderophores are microbial iron chelating agents that sequester physiologically essential iron for microbes. Conjugation of drugs to siderophores allows use of active iron transport for microbially directed drug delivery. Syntheses and biological studies are described of the first multidrug isocyanurate-based siderophore analogues separately containing one, two, and three 5-fluorouridine (5-FU) derivatives as the drug component. The results indicate that a single siderophore can be used to deliver multiple drugs to target pathogenic microorganisms.

摘要

铁载体是微生物铁螯合剂，可螯合微生物生理必需的铁。将药物与铁载体共轭可利用活性铁转运进行微生物靶向药物递送。本文描述了首个基于异三聚氰酸酯的多药铁载体类似物的合成及生物学研究，这些类似物分别含有一个、两个和三个5-氟尿苷（5-FU）衍生物作为药物成分。结果表明，单个铁载体可用于将多种药物递送至靶向致病微生物。