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Dihydropyrimidinones Against Multiresistant Bacteria
The increase in bacterial resistance to antimicrobials has led to high morbidity and mortality rates, posing a major public health problem, requiring the discovery of novel antimicrobial substances. The biological samples were identified as the Gram-negative bacilli Acinetobacter baumannii, Escheric...
Autores principales: | , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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Frontiers Media S.A.
2022
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8973396/ https://www.ncbi.nlm.nih.gov/pubmed/35369453 http://dx.doi.org/10.3389/fmicb.2022.743213 |
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author | Castro Jara, Marisa Silva, Allison Carlos Assunção Ritter, Marina da Silva, Adriana Fernandes Gonçalves, Carolina Lambrecht dos Santos, Pedro Rassier Borja, Luciano Sisconetto de Pereira, Cláudio Martin Pereira da Silva Nascente, Patrícia |
author_facet | Castro Jara, Marisa Silva, Allison Carlos Assunção Ritter, Marina da Silva, Adriana Fernandes Gonçalves, Carolina Lambrecht dos Santos, Pedro Rassier Borja, Luciano Sisconetto de Pereira, Cláudio Martin Pereira da Silva Nascente, Patrícia |
author_sort | Castro Jara, Marisa |
collection | PubMed |
description | The increase in bacterial resistance to antimicrobials has led to high morbidity and mortality rates, posing a major public health problem, requiring the discovery of novel antimicrobial substances. The biological samples were identified as the Gram-negative bacilli Acinetobacter baumannii, Escherichia coli, Enterobacter cloacae, Klebsiella pneumoniae, Morganella morgannii, Pseudomonas aeruginosa and Serratia marcescens and the Gram-positive cocci Enterococcus faecium, and Staphylococcus aureus, all of them resistant to at least three classes of antimicrobials. The antibacterial activity of the compounds was checked in vitro by determining the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) by the broth microdilution method and plating in brain heart infusion (BHI) agar, respectively. The chemical characterization of the compounds was performed by measuring the melting point and gas chromatography coupled with mass spectrometry (GC–MS) on a Shimadzu GC–MS-QP system 2010SE. Synthetic compounds showed antimicrobial activity against Gram-positive cocci at MIC concentrations 0.16–80 μg/ml and Gram-negative bacilli at MIC concentrations 23.2–80 μg/ml. Enterococcus faecium and S. aureus had the best MIC values. The results of the cytotoxicity test indicated that the synthetic compounds showed no significant difference in three concentrations tested (5, 20, and 80 μg/ml), allowing cell viability not different from that assigned to the control, without the tested compounds. In this context, the development of DHPM derivatives brings an alternative and perspective on effectiveness of drugs as potential future antimicrobial agents. |
format | Online Article Text |
id | pubmed-8973396 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | Frontiers Media S.A. |
record_format | MEDLINE/PubMed |
spelling | pubmed-89733962022-04-02 Dihydropyrimidinones Against Multiresistant Bacteria Castro Jara, Marisa Silva, Allison Carlos Assunção Ritter, Marina da Silva, Adriana Fernandes Gonçalves, Carolina Lambrecht dos Santos, Pedro Rassier Borja, Luciano Sisconetto de Pereira, Cláudio Martin Pereira da Silva Nascente, Patrícia Front Microbiol Microbiology The increase in bacterial resistance to antimicrobials has led to high morbidity and mortality rates, posing a major public health problem, requiring the discovery of novel antimicrobial substances. The biological samples were identified as the Gram-negative bacilli Acinetobacter baumannii, Escherichia coli, Enterobacter cloacae, Klebsiella pneumoniae, Morganella morgannii, Pseudomonas aeruginosa and Serratia marcescens and the Gram-positive cocci Enterococcus faecium, and Staphylococcus aureus, all of them resistant to at least three classes of antimicrobials. The antibacterial activity of the compounds was checked in vitro by determining the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) by the broth microdilution method and plating in brain heart infusion (BHI) agar, respectively. The chemical characterization of the compounds was performed by measuring the melting point and gas chromatography coupled with mass spectrometry (GC–MS) on a Shimadzu GC–MS-QP system 2010SE. Synthetic compounds showed antimicrobial activity against Gram-positive cocci at MIC concentrations 0.16–80 μg/ml and Gram-negative bacilli at MIC concentrations 23.2–80 μg/ml. Enterococcus faecium and S. aureus had the best MIC values. The results of the cytotoxicity test indicated that the synthetic compounds showed no significant difference in three concentrations tested (5, 20, and 80 μg/ml), allowing cell viability not different from that assigned to the control, without the tested compounds. In this context, the development of DHPM derivatives brings an alternative and perspective on effectiveness of drugs as potential future antimicrobial agents. Frontiers Media S.A. 2022-03-18 /pmc/articles/PMC8973396/ /pubmed/35369453 http://dx.doi.org/10.3389/fmicb.2022.743213 Text en Copyright © 2022 Castro Jara, Assunção Silva, Ritter, Fernandes da Silva, Lambrecht Gonçalves, Rassier dos Santos, Sisconetto Borja, Martin Pereira de Pereira and da Silva Nascente. https://creativecommons.org/licenses/by/4.0/This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms. |
spellingShingle | Microbiology Castro Jara, Marisa Silva, Allison Carlos Assunção Ritter, Marina da Silva, Adriana Fernandes Gonçalves, Carolina Lambrecht dos Santos, Pedro Rassier Borja, Luciano Sisconetto de Pereira, Cláudio Martin Pereira da Silva Nascente, Patrícia Dihydropyrimidinones Against Multiresistant Bacteria |
title | Dihydropyrimidinones Against Multiresistant Bacteria |
title_full | Dihydropyrimidinones Against Multiresistant Bacteria |
title_fullStr | Dihydropyrimidinones Against Multiresistant Bacteria |
title_full_unstemmed | Dihydropyrimidinones Against Multiresistant Bacteria |
title_short | Dihydropyrimidinones Against Multiresistant Bacteria |
title_sort | dihydropyrimidinones against multiresistant bacteria |
topic | Microbiology |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8973396/ https://www.ncbi.nlm.nih.gov/pubmed/35369453 http://dx.doi.org/10.3389/fmicb.2022.743213 |
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