Research output: Contribution to journal › Article › peer-review
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.Research output: Contribution to journal › Article › peer-review
}
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