Antimicrobial and anthelmintic activities of aryl urea agents

Result code in 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>

Alternative codes found

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

Result on the web

<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>

Result language

angličtina

Original language name

Antimicrobial and anthelmintic activities of aryl urea agents

Original language description

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.

Czech name

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Czech description

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Type

J_imp - Article in a specialist periodical, which is included in the Web of Science database

CEP classification

—

OECD FORD branch

10606 - Microbiology

Project

<a href="/en/project/LTC19030" target="_blank" >LTC19030: High-throughput screening for new anthelmintics</a><br>

Continuities

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Publication year

2023

Confidentiality

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

Name of the periodical

Journal of Global Antimicrobial Resistance

ISSN

2213-7165

e-ISSN

2213-7173

Volume of the periodical

33

Issue of the periodical within the volume

JUN

Country of publishing house

NL - THE KINGDOM OF THE NETHERLANDS

Number of pages

6

Pages from-to

114-119

UT code for WoS article

001054062100001

EID of the result in the Scopus database

2-s2.0-85151485296