Synthesis, iron(III)-binding affinity and in vitro evaluation of 3-hydroxypyridin-4-one hexadentate ligands as potential antimicrobial agents

被引:37
|
作者
Xu, Bo [1 ]
Kong, Xiao-Le [2 ]
Zhou, Tao [1 ]
Qiu, Di-Hong [3 ]
Chen, Yu-Lin [2 ]
Liu, Mu-Song [4 ]
Yang, Rong-Hua [1 ]
Hider, Robert C. [2 ]
机构
[1] Zhejiang Gongshang Univ, Sch Food Sci & Biotechnol, Hangzhou 310012, Zhejiang, Peoples R China
[2] Kings Coll London, Div Pharmaceut Sci, London SE1 9NH, England
[3] Ningbo Univ, Fac Life Sci & Biotechnol, Ningbo 315211, Zhejiang, Peoples R China
[4] Zhejiang Univ Technol, Coll Pharmaceut Sci, Hangzhou 310014, Zhejiang, Peoples R China
基金
中国国家自然科学基金;
关键词
Iron chelator; 3-Hydroxypyridin-4-one; Hexadentate; Antimicrobial activity; IRON CHELATORS; PHYSICOCHEMICAL PROPERTIES; BIOLOGICAL EVALUATION; BACTERIAL-GROWTH; INHIBITION; DESIGN; THALASSEMIA; THERAPY; ICL670;
D O I
10.1016/j.bmcl.2011.08.097
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Iron is a critical element for the survival of bacteria. We have designed and synthesized two novel 3-hydroxypyridin-4-one hexadentate ligands with high affinity for iron(III), which disrupt bacterial iron absorption. Biological studies demonstrate that these two chelators have significant inhibitory effect against both Gram-positive and Gram-negative bacteria, and therefore have potential as antimicrobial agents. (C) 2011 Elsevier Ltd. All rights reserved.
引用
收藏
页码:6376 / 6380
页数:5
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