铁转运介导的药物递送：三儿茶酚酸盐类铁载体-氨基青霉素缀合物的实用合成及体外抗菌研究揭示了对铜绿假单胞菌的选择性高效活性。
Iron transport-mediated drug delivery: practical syntheses and in vitro antibacterial studies of tris-catecholate siderophore-aminopenicillin conjugates reveals selectively potent antipseudomonal activity.
机构信息
Department of Chemistry and Biochemistry, University of Notre Dame, 251 Nieuwland Science Hall, Notre Dame, Indiana 46556, USA.
出版信息
J Am Chem Soc. 2012 Jun 20;134(24):9898-901. doi: 10.1021/ja303446w. Epub 2012 Jun 6.
Abstract
An artificial tris-catecolate siderophore with a tripodal backbone and its conjugates with ampicillin and amoxicillin were synthesized. Both conjugates exhibited significantly enhanced in vitro antibacterial activities against Gram-negative species compared to the parent drugs, especially against Pseudomonas aeruginosa . The conjugates appeared to be assimilated by an induced bacterial iron transport process as their activities were inversely related to iron concentration. The easily synthesized tris-catecolate siderophore has great potential for future development of various drug conjugates to target antibiotic-resistant Gram-negative bacteria.
摘要
合成了一种具有三足骨架的人工三儿茶酚酸盐类铁载体及其与氨苄西林和阿莫西林的轭合物。与母体药物相比，这两种轭合物对革兰氏阴性菌的体外抗菌活性均显著增强，尤其是对铜绿假单胞菌。这些轭合物似乎通过诱导的细菌铁转运过程被吸收，因为它们的活性与铁浓度呈反比。这种易于合成的三儿茶酚酸盐类铁载体具有很大的潜力，可用于开发针对抗药性革兰氏阴性菌的各种药物轭合物。
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Iron transport-mediated drug delivery: practical syntheses and in vitro antibacterial studies of tris-catecholate siderophore-aminopenicillin conjugates reveals selectively potent antipseudomonal activity.铁转运介导的药物递送：三儿茶酚酸盐类铁载体-氨基青霉素缀合物的实用合成及体外抗菌研究揭示了对铜绿假单胞菌的选择性高效活性。
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