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Antibacterial activity and mechanism of action of a thiophenyl substituted pyrimidine derivative
The issue of multidrug resistant bacteria is a worldwide health threat. To develop new antibacterial agents with new mechanisms of action is thus an urgent request to address this antibiotic resistance crisis. In the present study, a new thiophenyl-pyrimidine derivative was prepared and utilized as...
Autores principales: | , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
The Royal Society of Chemistry
2019
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9062536/ https://www.ncbi.nlm.nih.gov/pubmed/35515309 http://dx.doi.org/10.1039/c9ra01001g |
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author | Fang, Zhiyuan Li, Yanan Zheng, Yuanyuan Li, Xiaomei Lu, Yu-Jing Yan, Siu-Cheong Wong, Wing-Leung Chan, Kin-Fai Wong, Kwok-yin Sun, Ning |
author_facet | Fang, Zhiyuan Li, Yanan Zheng, Yuanyuan Li, Xiaomei Lu, Yu-Jing Yan, Siu-Cheong Wong, Wing-Leung Chan, Kin-Fai Wong, Kwok-yin Sun, Ning |
author_sort | Fang, Zhiyuan |
collection | PubMed |
description | The issue of multidrug resistant bacteria is a worldwide health threat. To develop new antibacterial agents with new mechanisms of action is thus an urgent request to address this antibiotic resistance crisis. In the present study, a new thiophenyl-pyrimidine derivative was prepared and utilized as an effective antibacterial agent against Gram-positive strains. In the tests against MRSA and VREs, the compound showed higher antibacterial potency than that of vancomycin and methicillin. The mode of action is probably attributed to the effective inhibition of FtsZ polymerization, GTPase activity, and bacterial cell division, which cause bactericidal effects. The compound could be a potential candidate for further development as an effective antibiotic to combat drug-resistant bacteria. |
format | Online Article Text |
id | pubmed-9062536 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2019 |
publisher | The Royal Society of Chemistry |
record_format | MEDLINE/PubMed |
spelling | pubmed-90625362022-05-04 Antibacterial activity and mechanism of action of a thiophenyl substituted pyrimidine derivative Fang, Zhiyuan Li, Yanan Zheng, Yuanyuan Li, Xiaomei Lu, Yu-Jing Yan, Siu-Cheong Wong, Wing-Leung Chan, Kin-Fai Wong, Kwok-yin Sun, Ning RSC Adv Chemistry The issue of multidrug resistant bacteria is a worldwide health threat. To develop new antibacterial agents with new mechanisms of action is thus an urgent request to address this antibiotic resistance crisis. In the present study, a new thiophenyl-pyrimidine derivative was prepared and utilized as an effective antibacterial agent against Gram-positive strains. In the tests against MRSA and VREs, the compound showed higher antibacterial potency than that of vancomycin and methicillin. The mode of action is probably attributed to the effective inhibition of FtsZ polymerization, GTPase activity, and bacterial cell division, which cause bactericidal effects. The compound could be a potential candidate for further development as an effective antibiotic to combat drug-resistant bacteria. The Royal Society of Chemistry 2019-04-05 /pmc/articles/PMC9062536/ /pubmed/35515309 http://dx.doi.org/10.1039/c9ra01001g Text en This journal is © The Royal Society of Chemistry https://creativecommons.org/licenses/by-nc/3.0/ |
spellingShingle | Chemistry Fang, Zhiyuan Li, Yanan Zheng, Yuanyuan Li, Xiaomei Lu, Yu-Jing Yan, Siu-Cheong Wong, Wing-Leung Chan, Kin-Fai Wong, Kwok-yin Sun, Ning Antibacterial activity and mechanism of action of a thiophenyl substituted pyrimidine derivative |
title | Antibacterial activity and mechanism of action of a thiophenyl substituted pyrimidine derivative |
title_full | Antibacterial activity and mechanism of action of a thiophenyl substituted pyrimidine derivative |
title_fullStr | Antibacterial activity and mechanism of action of a thiophenyl substituted pyrimidine derivative |
title_full_unstemmed | Antibacterial activity and mechanism of action of a thiophenyl substituted pyrimidine derivative |
title_short | Antibacterial activity and mechanism of action of a thiophenyl substituted pyrimidine derivative |
title_sort | antibacterial activity and mechanism of action of a thiophenyl substituted pyrimidine derivative |
topic | Chemistry |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9062536/ https://www.ncbi.nlm.nih.gov/pubmed/35515309 http://dx.doi.org/10.1039/c9ra01001g |
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