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Conjugates of Iron-Transporting N-Hydroxylactams with Ciprofloxacin. / Bakulina, Olga; Bannykh, Anton; Levashova, Ekaterina; Krasavin, Mikhail.

In: Molecules, Vol. 27, No. 12, 3910, 18.06.2022.

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@article{9a7fe24793614828952ab79b1f4efe9f,
title = "Conjugates of Iron-Transporting N-Hydroxylactams with Ciprofloxacin",
abstract = "Screening of a library of novel N-hydroxylactams amenable by the Castagnoli-Cushman reaction identified four lead compounds that facilitated55Fe transport into P. aeruginosa cells (one of these synthetic siderophores was found to be as efficient at promoting iron uptake as the natural siderophores pyoverdine, pyochelin or enterobactin). Conjugates of the four lead siderophores with ciprofloxacin were tested for antibacterial activity against P. aeruginosa POA1 (wild type) and the ∆pvdF∆pchA mutant strain. The antibacterial activity was found to be pronounced against the ∆pvdF∆pchA mutant strain grown in CAA medium but not for the POA1 strain. This may be indic-ative of these compounds being {\textquoteleft}Trojan horse{\textquoteright} antibiotics. Further scrutiny of the mechanism of the antibacterial action of the newly developed conjugates is warranted.",
keywords = "bacterial iron transport, Castagnoli-Cushman reaction, cyclic hydroxamic acids, siderophores, Trojan horse antibiotics",
author = "Olga Bakulina and Anton Bannykh and Ekaterina Levashova and Mikhail Krasavin",
note = "Publisher Copyright: {\textcopyright} 2022 by the authors. Licensee MDPI, Basel, Switzerland.",
year = "2022",
month = jun,
day = "18",
doi = "10.3390/molecules27123910",
language = "English",
volume = "27",
journal = "Molecules",
issn = "1420-3049",
publisher = "MDPI AG",
number = "12",

}

RIS

TY - JOUR

T1 - Conjugates of Iron-Transporting N-Hydroxylactams with Ciprofloxacin

AU - Bakulina, Olga

AU - Bannykh, Anton

AU - Levashova, Ekaterina

AU - Krasavin, Mikhail

N1 - Publisher Copyright: © 2022 by the authors. Licensee MDPI, Basel, Switzerland.

PY - 2022/6/18

Y1 - 2022/6/18

N2 - Screening of a library of novel N-hydroxylactams amenable by the Castagnoli-Cushman reaction identified four lead compounds that facilitated55Fe transport into P. aeruginosa cells (one of these synthetic siderophores was found to be as efficient at promoting iron uptake as the natural siderophores pyoverdine, pyochelin or enterobactin). Conjugates of the four lead siderophores with ciprofloxacin were tested for antibacterial activity against P. aeruginosa POA1 (wild type) and the ∆pvdF∆pchA mutant strain. The antibacterial activity was found to be pronounced against the ∆pvdF∆pchA mutant strain grown in CAA medium but not for the POA1 strain. This may be indic-ative of these compounds being ‘Trojan horse’ antibiotics. Further scrutiny of the mechanism of the antibacterial action of the newly developed conjugates is warranted.

AB - Screening of a library of novel N-hydroxylactams amenable by the Castagnoli-Cushman reaction identified four lead compounds that facilitated55Fe transport into P. aeruginosa cells (one of these synthetic siderophores was found to be as efficient at promoting iron uptake as the natural siderophores pyoverdine, pyochelin or enterobactin). Conjugates of the four lead siderophores with ciprofloxacin were tested for antibacterial activity against P. aeruginosa POA1 (wild type) and the ∆pvdF∆pchA mutant strain. The antibacterial activity was found to be pronounced against the ∆pvdF∆pchA mutant strain grown in CAA medium but not for the POA1 strain. This may be indic-ative of these compounds being ‘Trojan horse’ antibiotics. Further scrutiny of the mechanism of the antibacterial action of the newly developed conjugates is warranted.

KW - bacterial iron transport

KW - Castagnoli-Cushman reaction

KW - cyclic hydroxamic acids

KW - siderophores

KW - Trojan horse antibiotics

UR - http://www.scopus.com/inward/record.url?scp=85132822257&partnerID=8YFLogxK

UR - https://www.mendeley.com/catalogue/fea3c8e6-71a5-319b-9289-e524bcca5513/

U2 - 10.3390/molecules27123910

DO - 10.3390/molecules27123910

M3 - Article

C2 - 35745033

AN - SCOPUS:85132822257

VL - 27

JO - Molecules

JF - Molecules

SN - 1420-3049

IS - 12

M1 - 3910

ER -

ID: 97069714