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N-benzyl derivatives of long-chained 4-Amino-7-chloro-quionolines as inhibitors of pyocyanin production in Pseudomonas aeruginosa

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2019
N-Benzyl_Derivatives_acc_2019.pdf (1.198Mb)
Authors
Aleksic, Ivana
Jeremić, Jelena
Milivojevic, Dusan
Ilić-Tomić, Tatjana
Šegan, Sandra
Zlatović, Mario
Opsenica, Dejan
Senerovic, Lidija
Article (Accepted Version)
,
American Chemical Society
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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.
Keywords:
Long-Chained 4-Amino-7-chloro-quionolines / Pseudomonas aeruginosa / quorum sensing / Inhibitors of Pyocyanin
Source:
ACS Chemical Biology, 2019, 14, 12, 2800-2809
Publisher:
  • American Chemical Society
Projects:
  • The synthesis of aminoquinoline-based antimalarials and botulinum neurotoxin A inhibitors (RS-172008)
  • Microbial diversity study and characterization of beneficial environmental microorganisms (RS-173048)
Note:
  • 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

DOI: 10.1021/acschembio.9b00682

ISSN: 1554-8929

PubMed: 31647218

WoS: 000504806100033

Scopus: 2-s2.0-85074933821
[ Google Scholar ]
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URI
http://cer.ihtm.bg.ac.rs/handle/123456789/3198
http://cer.ihtm.bg.ac.rs/handle/123456789/3341
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  • Radovi istraživača / Researchers' publications
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