Antimicrobial and anthelmintic activities of aryl urea agents

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61389030%3A_____%2F23%3A00578552" target="_blank" >RIV/61389030:_____/23:00578552 - isvavai.cz</a>

Nalezeny alternativní kódy

RIV/61989592:15110/23:73619598 RIV/61989592:15310/23:73619598

Výsledek na webu

<a href="https://doi.org/10.1016/j.jgar.2023.02.021" target="_blank" >https://doi.org/10.1016/j.jgar.2023.02.021</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.jgar.2023.02.021" target="_blank" >10.1016/j.jgar.2023.02.021</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Antimicrobial and anthelmintic activities of aryl urea agents

Popis výsledku v původním jazyce

Objectives: This study aimed to characterise compounds with activity against carbapenemase-expressing Gram-negative bacteria and nematodes and evaluate their cytotoxicity to non-cancerous human cells. Methods: The antimicrobial activity and toxicity of a series of phenyl-substituted urea derivatives were evaluated using broth microdilution, chitinase, and resazurin reduction assays. Results: The effects of different substitutions present on the nitrogen atoms of the urea backbone were investigated. Several compounds were active against Staphylococcus aureus and Escherichia coli control strains. Specifically, derivatives 7b, 11b, and 67d exhibited antimicrobial activity against Klebsiella pneumoniae 16, a carbapenemase-producing Enterobacteriaceae species, with minimum inhibitory concentration (MIC) values of 100, 50, and 72 µM (32, 64, and 32 mg/L), respectively. In addition, the MICs obtained against a multidrug-resistant E. coli strain were 100, 50, and 36 µM (32, 16, and 16 mg/L) for the same compounds, respectively. Furthermore, the urea derivatives 18b, 29b, 50c, 51c, 52c, 55c–59c, and 62c were very active towards the nematode Caenorhabditis elegans. Conclusions: Testing on non-cancerous human cell lines suggested that some of the compounds have the potential to affect bacteria, especially helminths, with limited cytotoxicity to humans. Given the simplicity of synthesis for this class of compounds and their potency against Gram-negative, carbapenemase-expressing K. pneumoniae, aryl ureas possessing the 3,5-dichloro-phenyl group certainly warrant further investigation to exploit their selectivity.

Název v anglickém jazyce

Antimicrobial and anthelmintic activities of aryl urea agents

Popis výsledku anglicky

Objectives: This study aimed to characterise compounds with activity against carbapenemase-expressing Gram-negative bacteria and nematodes and evaluate their cytotoxicity to non-cancerous human cells. Methods: The antimicrobial activity and toxicity of a series of phenyl-substituted urea derivatives were evaluated using broth microdilution, chitinase, and resazurin reduction assays. Results: The effects of different substitutions present on the nitrogen atoms of the urea backbone were investigated. Several compounds were active against Staphylococcus aureus and Escherichia coli control strains. Specifically, derivatives 7b, 11b, and 67d exhibited antimicrobial activity against Klebsiella pneumoniae 16, a carbapenemase-producing Enterobacteriaceae species, with minimum inhibitory concentration (MIC) values of 100, 50, and 72 µM (32, 64, and 32 mg/L), respectively. In addition, the MICs obtained against a multidrug-resistant E. coli strain were 100, 50, and 36 µM (32, 16, and 16 mg/L) for the same compounds, respectively. Furthermore, the urea derivatives 18b, 29b, 50c, 51c, 52c, 55c–59c, and 62c were very active towards the nematode Caenorhabditis elegans. Conclusions: Testing on non-cancerous human cell lines suggested that some of the compounds have the potential to affect bacteria, especially helminths, with limited cytotoxicity to humans. Given the simplicity of synthesis for this class of compounds and their potency against Gram-negative, carbapenemase-expressing K. pneumoniae, aryl ureas possessing the 3,5-dichloro-phenyl group certainly warrant further investigation to exploit their selectivity.

Druh

J_imp - Článek v periodiku v databázi Web of Science

CEP obor

—

OECD FORD obor

10606 - Microbiology

Projekt

<a href="/cs/project/LTC19030" target="_blank" >LTC19030: Vysokokapacitní vyhledávání nových anthelmintik</a><br>

Návaznosti

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Rok uplatnění

2023

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

Journal of Global Antimicrobial Resistance

ISSN

2213-7165

e-ISSN

2213-7173

Svazek periodika

33

Číslo periodika v rámci svazku

JUN

Stát vydavatele periodika

NL - Nizozemsko

Počet stran výsledku

6

Strana od-do

114-119

Kód UT WoS článku

001054062100001

EID výsledku v databázi Scopus

2-s2.0-85151485296