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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.
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页码:6376 / 6380
页数:5
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