TY  - JOUR
AU  - Aleksić, Ivana
AU  - Jeremić, Jelena
AU  - Milivojević, Dušan
AU  - Ilić-Tomić, Tatjana
AU  - Segan, Sandra
AU  - Zlatović, Mario
AU  - Opsenica, Dejan M.
AU  - Šenerović, Lidija
PY  - 2019
UR  - https://imagine.imgge.bg.ac.rs/handle/123456789/1225
AB  - 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 mu M), biofilm formation (BFIC50 = 50 mu M), and motility. Experimentally, the compound's activity is achieved through competitive inhibition of PqsR, and structure-activity data were rationalized using molecular docking studies.
PB  - Amer Chemical Soc, Washington
T2  - Acs Chemical Biology
T1  - N-Benzyl Derivatives of Long-Chained 4-Amino-7-chloro-quionolines as Inhibitors of Pyocyanin Production in Pseudomonas aeruginosa
EP  - 2809
IS  - 12
SP  - 2800
VL  - 14
DO  - 10.1021/acschembio.9b00682
ER  - 

@article{
author = "Aleksić, Ivana and Jeremić, Jelena and Milivojević, Dušan and Ilić-Tomić, Tatjana and Segan, Sandra and Zlatović, Mario and Opsenica, Dejan M. and Šenerović, Lidija",
year = "2019",
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 mu M), biofilm formation (BFIC50 = 50 mu M), and motility. Experimentally, the compound's activity is achieved through competitive inhibition of PqsR, and structure-activity data were rationalized using molecular docking studies.",
publisher = "Amer Chemical Soc, Washington",
journal = "Acs Chemical Biology",
title = "N-Benzyl Derivatives of Long-Chained 4-Amino-7-chloro-quionolines as Inhibitors of Pyocyanin Production in Pseudomonas aeruginosa",
pages = "2809-2800",
number = "12",
volume = "14",
doi = "10.1021/acschembio.9b00682"
}

Aleksić, I., Jeremić, J., Milivojević, D., Ilić-Tomić, T., Segan, S., Zlatović, M., Opsenica, D. M.,& Šenerović, L.. (2019). N-Benzyl Derivatives of Long-Chained 4-Amino-7-chloro-quionolines as Inhibitors of Pyocyanin Production in Pseudomonas aeruginosa. in Acs Chemical Biology
Amer Chemical Soc, Washington., 14(12), 2800-2809.
https://doi.org/10.1021/acschembio.9b00682

Aleksić I, Jeremić J, Milivojević D, Ilić-Tomić T, Segan S, Zlatović M, Opsenica DM, Šenerović L. N-Benzyl Derivatives of Long-Chained 4-Amino-7-chloro-quionolines as Inhibitors of Pyocyanin Production in Pseudomonas aeruginosa. in Acs Chemical Biology. 2019;14(12):2800-2809.
doi:10.1021/acschembio.9b00682 .

Aleksić, Ivana, Jeremić, Jelena, Milivojević, Dušan, Ilić-Tomić, Tatjana, Segan, Sandra, Zlatović, Mario, Opsenica, Dejan M., Šenerović, Lidija, "N-Benzyl Derivatives of Long-Chained 4-Amino-7-chloro-quionolines as Inhibitors of Pyocyanin Production in Pseudomonas aeruginosa" in Acs Chemical Biology, 14, no. 12 (2019):2800-2809,
https://doi.org/10.1021/acschembio.9b00682 . .