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

Thumbnail
2019
N-Benzyl_Derivatives_acc_2019.pdf (1.198Mb)
Аутори
Aleksic, Ivana
Jeremić, Jelena
Milivojevic, Dusan
Ilić-Tomić, Tatjana
Šegan, Sandra
Zlatović, Mario
Opsenica, Dejan
Senerovic, Lidija
Чланак у часопису (Рецензирана верзија)
,
American Chemical Society (ACS)
Метаподаци
Приказ свих података о документу
Апстракт
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.
Кључне речи:
Long-Chained 4-Amino-7-chloro-quionolines / Pseudomonas aeruginosa / quorum sensing / Inhibitors of Pyocyanin
Извор:
ACS Chemical Biology, 2019, 14, 12, 2800-2809
Издавач:
  • American Chemical Society (ACS)
Пројекти:
  • Синтеза аминохинолина и њихових деривата као антималарика и инхибитора ботулинум неуротоксина А (RS-172008)
  • Изучавање микробиолошког диверзитета и карактеризација корисних срединских микроорганизама (RS-173048)
Напомена:
  • 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 ]
2
2
URI
http://cer.ihtm.bg.ac.rs/handle/123456789/3198
http://cer.ihtm.bg.ac.rs/handle/123456789/3341
Колекције
  • Radovi istraživača / Researchers' publications
Институција
IHTM
TY  - JOUR
AU  - Aleksic, Ivana
AU  - Jeremić, Jelena
AU  - Milivojevic, Dusan
AU  - Ilić-Tomić, Tatjana
AU  - Šegan, Sandra
AU  - Zlatović, Mario
AU  - Opsenica, Dejan
AU  - Senerovic, Lidija
PY  - 2019
UR  - http://cer.ihtm.bg.ac.rs/handle/123456789/3198
UR  - http://cer.ihtm.bg.ac.rs/handle/123456789/3341
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 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.
PB  - American Chemical Society (ACS)
T2  - ACS Chemical Biology
T1  - N-benzyl derivatives of long-chained 4-Amino-7-chloro-quionolines as inhibitors of pyocyanin production in Pseudomonas aeruginosa
VL  - 14
IS  - 12
SP  - 2800
EP  - 2809
DO  - 10.1021/acschembio.9b00682
ER  - 
@article{
author = "Aleksic, Ivana and Jeremić, Jelena and Milivojevic, Dusan and Ilić-Tomić, Tatjana and Šegan, Sandra and Zlatović, Mario and Opsenica, Dejan and Senerovic, Lidija",
year = "2019",
url = "http://cer.ihtm.bg.ac.rs/handle/123456789/3198, http://cer.ihtm.bg.ac.rs/handle/123456789/3341",
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.",
publisher = "American Chemical Society (ACS)",
journal = "ACS Chemical Biology",
title = "N-benzyl derivatives of long-chained 4-Amino-7-chloro-quionolines as inhibitors of pyocyanin production in Pseudomonas aeruginosa",
volume = "14",
number = "12",
pages = "2800-2809",
doi = "10.1021/acschembio.9b00682"
}
Aleksic I, Jeremić J, Milivojevic D, Ilić-Tomić T, Šegan S, Zlatović M, Opsenica D, Senerovic L. N-benzyl derivatives of long-chained 4-Amino-7-chloro-quionolines as inhibitors of pyocyanin production in Pseudomonas aeruginosa. ACS Chemical Biology. 2019;14(12):2800-2809
Aleksic, I., Jeremić, J., Milivojevic, D., Ilić-Tomić, T., Šegan, S., Zlatović, M., Opsenica, D.,& Senerovic, L. (2019). N-benzyl derivatives of long-chained 4-Amino-7-chloro-quionolines as inhibitors of pyocyanin production in Pseudomonas aeruginosa.
ACS Chemical BiologyAmerican Chemical Society (ACS)., 14(12), 2800-2809.
https://doi.org/10.1021/acschembio.9b00682
Aleksic Ivana, Jeremić Jelena, Milivojevic Dusan, Ilić-Tomić Tatjana, Šegan Sandra, Zlatović Mario, Opsenica Dejan, Senerovic Lidija, "N-benzyl derivatives of long-chained 4-Amino-7-chloro-quionolines as inhibitors of pyocyanin production in Pseudomonas aeruginosa" 14, no. 12 (2019):2800-2809,
https://doi.org/10.1021/acschembio.9b00682 .

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