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ACS Chemical Biology
Article . 2019 . Peer-reviewed
License: STM Policy #29
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n benzyl derivatives of long chained 4 amino 7 chloro quionolines as inhibitors of pyocyanin production in pseudomonas aeruginosa

Authors: Ivana Aleksic; Jelena Jeremic; Dusan Milivojevic; Tatjana Ilic-Tomic; Sandra Šegan; Mario Zlatović; Dejan M. Opsenica; +1 Authors

n benzyl derivatives of long chained 4 amino 7 chloro quionolines as inhibitors of pyocyanin production in pseudomonas aeruginosa

Abstract

Pseudomonas aeruginosa is a leading cause of nosocomial infections that are becoming increasingly difficult to treat due to the occurrence of antibiotic resistant strains. Since P. aeruginosa virulence is controlled through quorum sensing, small molecule treatments inhibiting quorum sensing signaling pathways provide a promising therapeutic option. Consequently, we synthesized a series of N-octaneamino-4-aminoquinoline derivatives to optimize this chemotype’s antivirulence activity against P. aeruginosa via inhibition of pyocyanin production. The most potent derivative, which possesses a benzofuran substituent, provided effective inhibition of pyocyanin production (IC50 = 12 μM), biofilm formation (BFIC50 = 50 μM), and motility. Experimentally, the compound’s activity is achieved through competitive inhibition of PqsR, and structure–activity data were rationalized using molecular docking studies.

This is the peer-reviewed version of the article: Ivana Aleksic, Jelena Jeremic, Dusan Milivojevic, Tatjana Ilic-Tomic, Sandra Šegan, Mario Zlatović, Dejan M. Opsenica, Lidija Senerovic, ACS Chem. Biol. 2019, 14, 12, 2800-2809, [https://doi.org/10.1021/acschembio.9b00682]

The published version: [http://cer.ihtm.bg.ac.rs/handle/123456789/3198]

Country
Serbia
Keywords

Inhibitors of Pyocyanin, Pseudomonas aeruginosa, Long-Chained 4-Amino-7-chloro-quionolines, quorum sensing

  • BIP!
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    This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
    25
    popularity
    This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
    Top 10%
    influence
    This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
    Average
    impulse
    This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
    Top 10%
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citations
This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Citations provided by BIP!
popularity
This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
BIP!Popularity provided by BIP!
influence
This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Influence provided by BIP!
impulse
This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
BIP!Impulse provided by BIP!
25
Top 10%
Average
Top 10%
Green
bronze