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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...

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Autores principales: 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
Formato: Online Artículo Texto
Lenguaje:English
Publicado: The Royal Society of Chemistry 2019
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.
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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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