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Synthesis, iron binding and antimicrobial properties of hexadentate 3-hydroxypyridinones-terminated dendrimers
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2018-05-30 , DOI: 10.1016/j.bmcl.2018.05.058
Tao Zhou , Kai Chen , Li-Min Kong , Mu-Song Liu , Yong-Min Ma , Yuan-Yuan Xie , Robert C. Hider

Macromolecular chelators have potential applications in the medical area, for instance, in treatment of iron overload-related disorders and in the treatment of external infections. In this investigation, several novel iron(III)-selective hydroxypyridinone hexadentate-terminated first and second generation dendrimeric chelators were synthesized using a convergent strategy. Their iron chelating ability was demonstrated by UV/Visible spectrometry and high resolution mass spectrometry (HRMS). The iron binding affinities were also investigated by the competition with a fluorescent iron chelator CP691. The result indicated that these dendrimers possesses a high affinity for iron with a very high pFe3+ value, which is close to that of an isolated hexadentate unit. These dendrimeric chelators were found to exhibit inhibitory effect on the growth of both Gram-positive and Gram-negative bacteria.



中文翻译:

六齿3-羟基吡啶酮终止的树枝状大分子的合成,铁结合和抗菌性能

大分子螯合剂在医学领域具有潜在的应用,例如,在治疗与铁超负荷有关的疾病和治疗外部感染方面。在这项研究中,使用收敛策略合成了几种新颖的铁(III)-选择性羟基吡啶酮六齿终止的第一代和第二代树枝状螯合剂。紫外/可见光谱和高分辨率质谱(HRMS)证明了它们的铁螯合能力。还通过与荧光铁螯合剂CP691的竞争研究了铁的结合亲和力。结果表明,这些树枝状分子对铁具有很高的亲和力,具有很高的pFe 3+值,接近隔离的六齿单元的值。发现这些树枝状螯合剂对革兰氏阳性和革兰氏阴性细菌的生长均表现出抑制作用。

更新日期:2018-05-30
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