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Synthesis and in-vitro antimicrobial evaluation of a high-affinity iron chelator in combination with chloramphenicol

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Synthesis and in-vitro antimicrobial evaluation of a high-affinity iron chelator in combination with chloramphenicol. / Zhu, Chun Feng; Qiu, Di Hong; Kong, Xiao; Hider, Robert C.; Zhou, Tao.

In: Journal of Pharmacy and Pharmacology, Vol. 65, No. 4, 04.2013, p. 512-520.

Research output: Contribution to journalArticle

Harvard

Zhu, CF, Qiu, DH, Kong, X, Hider, RC & Zhou, T 2013, 'Synthesis and in-vitro antimicrobial evaluation of a high-affinity iron chelator in combination with chloramphenicol', Journal of Pharmacy and Pharmacology, vol. 65, no. 4, pp. 512-520. https://doi.org/10.1111/jphp.12013

APA

Zhu, C. F., Qiu, D. H., Kong, X., Hider, R. C., & Zhou, T. (2013). Synthesis and in-vitro antimicrobial evaluation of a high-affinity iron chelator in combination with chloramphenicol. Journal of Pharmacy and Pharmacology, 65(4), 512-520. https://doi.org/10.1111/jphp.12013

Vancouver

Zhu CF, Qiu DH, Kong X, Hider RC, Zhou T. Synthesis and in-vitro antimicrobial evaluation of a high-affinity iron chelator in combination with chloramphenicol. Journal of Pharmacy and Pharmacology. 2013 Apr;65(4):512-520. https://doi.org/10.1111/jphp.12013

Author

Zhu, Chun Feng ; Qiu, Di Hong ; Kong, Xiao ; Hider, Robert C. ; Zhou, Tao. / Synthesis and in-vitro antimicrobial evaluation of a high-affinity iron chelator in combination with chloramphenicol. In: Journal of Pharmacy and Pharmacology. 2013 ; Vol. 65, No. 4. pp. 512-520.

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@article{173f7d8498bd4e57a46e236d639ad1c3,
title = "Synthesis and in-vitro antimicrobial evaluation of a high-affinity iron chelator in combination with chloramphenicol",
abstract = "Objectives The objectives of this study were first to design and synthesize a hexadentate chelator with high iron(III) affinity and, second, to evaluate its antimicrobial activity in the presence and absence of chloramphenicol. Methods A hexadentate ligand was synthesized by conjugating a protected bidentate compound onto a tripodal structure. The pKa values and iron affinity of the chelator were determined by spectophotometric titration. Minimum inhibitory concentrations were determined by visual inspection of broth turbidity. The bactericidal rates were calculated by counting the colony numbers on a light board after incubation with and without an antimicrobial agent. Key findings A hexadentate 3-hydroxypyridin-4-one was found to possess a high affinity for iron(III), with a pFe value of 31.2 (negative logarithm of concentration of the free iron(III) in solution (when [Fe3+] Total = 10-6m; [Ligand]Total = 10 -5m; pH = 7.4). We found that this chelator had an appreciable inhibitory effect in vitro against the two bacterial strains Providencia stuartii and Staphylococcus aureus, particularly in the presence of chloramphenicol. Conclusions A 3-hydroxypyridin-4-one hexadentate ligand has potential as an antimicrobial agent. Combination therapy with this iron chelator plus chloramphenicol has potential for the treatment of extracellular infections.",
keywords = "3-hydroxypyridin-4-one, antimicrobial activity, chloramphenicol, hexadentate, iron chelator",
author = "Zhu, {Chun Feng} and Qiu, {Di Hong} and Xiao Kong and Hider, {Robert C.} and Tao Zhou",
year = "2013",
month = "4",
doi = "10.1111/jphp.12013",
language = "English",
volume = "65",
pages = "512--520",
journal = "Journal of Pharmacy and Pharmacology",
issn = "0022-3573",
publisher = "Wiley-Blackwell",
number = "4",

}

RIS (suitable for import to EndNote) Download

TY - JOUR

T1 - Synthesis and in-vitro antimicrobial evaluation of a high-affinity iron chelator in combination with chloramphenicol

AU - Zhu, Chun Feng

AU - Qiu, Di Hong

AU - Kong, Xiao

AU - Hider, Robert C.

AU - Zhou, Tao

PY - 2013/4

Y1 - 2013/4

N2 - Objectives The objectives of this study were first to design and synthesize a hexadentate chelator with high iron(III) affinity and, second, to evaluate its antimicrobial activity in the presence and absence of chloramphenicol. Methods A hexadentate ligand was synthesized by conjugating a protected bidentate compound onto a tripodal structure. The pKa values and iron affinity of the chelator were determined by spectophotometric titration. Minimum inhibitory concentrations were determined by visual inspection of broth turbidity. The bactericidal rates were calculated by counting the colony numbers on a light board after incubation with and without an antimicrobial agent. Key findings A hexadentate 3-hydroxypyridin-4-one was found to possess a high affinity for iron(III), with a pFe value of 31.2 (negative logarithm of concentration of the free iron(III) in solution (when [Fe3+] Total = 10-6m; [Ligand]Total = 10 -5m; pH = 7.4). We found that this chelator had an appreciable inhibitory effect in vitro against the two bacterial strains Providencia stuartii and Staphylococcus aureus, particularly in the presence of chloramphenicol. Conclusions A 3-hydroxypyridin-4-one hexadentate ligand has potential as an antimicrobial agent. Combination therapy with this iron chelator plus chloramphenicol has potential for the treatment of extracellular infections.

AB - Objectives The objectives of this study were first to design and synthesize a hexadentate chelator with high iron(III) affinity and, second, to evaluate its antimicrobial activity in the presence and absence of chloramphenicol. Methods A hexadentate ligand was synthesized by conjugating a protected bidentate compound onto a tripodal structure. The pKa values and iron affinity of the chelator were determined by spectophotometric titration. Minimum inhibitory concentrations were determined by visual inspection of broth turbidity. The bactericidal rates were calculated by counting the colony numbers on a light board after incubation with and without an antimicrobial agent. Key findings A hexadentate 3-hydroxypyridin-4-one was found to possess a high affinity for iron(III), with a pFe value of 31.2 (negative logarithm of concentration of the free iron(III) in solution (when [Fe3+] Total = 10-6m; [Ligand]Total = 10 -5m; pH = 7.4). We found that this chelator had an appreciable inhibitory effect in vitro against the two bacterial strains Providencia stuartii and Staphylococcus aureus, particularly in the presence of chloramphenicol. Conclusions A 3-hydroxypyridin-4-one hexadentate ligand has potential as an antimicrobial agent. Combination therapy with this iron chelator plus chloramphenicol has potential for the treatment of extracellular infections.

KW - 3-hydroxypyridin-4-one

KW - antimicrobial activity

KW - chloramphenicol

KW - hexadentate

KW - iron chelator

UR - http://www.scopus.com/inward/record.url?scp=84875245632&partnerID=8YFLogxK

U2 - 10.1111/jphp.12013

DO - 10.1111/jphp.12013

M3 - Article

C2 - 23488779

AN - SCOPUS:84875245632

VL - 65

SP - 512

EP - 520

JO - Journal of Pharmacy and Pharmacology

JF - Journal of Pharmacy and Pharmacology

SN - 0022-3573

IS - 4

ER -

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