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Potential of 2-Chloro-N-(4-fluoro-3-nitrophenyl)acetamide Against Klebsiella pneumoniae and In Vitro Toxicity Analysis

Klebsiella pneumoniae causes a wide range of community and nosocomial infections. The high capacity of this pathogen to acquire resistance drugs makes it necessary to develop therapeutic alternatives, discovering new antibacterial molecules. Acetamides are molecules that have several biological acti...

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Autores principales: Cordeiro, Laísa, Diniz-Neto, Hermes, Figueiredo, Pedro, Souza, Helivaldo, Sousa, Aleson, Andrade-Júnior, Francisco, Melo, Thamara, Ferreira, Elba, Oliveira, Rafael, Athayde-Filho, Petrônio, Barbosa-Filho, José, Oliveira-Filho, Abrahão, Lima, Edeltrudes
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7504751/
https://www.ncbi.nlm.nih.gov/pubmed/32877986
http://dx.doi.org/10.3390/molecules25173959
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author Cordeiro, Laísa
Diniz-Neto, Hermes
Figueiredo, Pedro
Souza, Helivaldo
Sousa, Aleson
Andrade-Júnior, Francisco
Melo, Thamara
Ferreira, Elba
Oliveira, Rafael
Athayde-Filho, Petrônio
Barbosa-Filho, José
Oliveira-Filho, Abrahão
Lima, Edeltrudes
author_facet Cordeiro, Laísa
Diniz-Neto, Hermes
Figueiredo, Pedro
Souza, Helivaldo
Sousa, Aleson
Andrade-Júnior, Francisco
Melo, Thamara
Ferreira, Elba
Oliveira, Rafael
Athayde-Filho, Petrônio
Barbosa-Filho, José
Oliveira-Filho, Abrahão
Lima, Edeltrudes
author_sort Cordeiro, Laísa
collection PubMed
description Klebsiella pneumoniae causes a wide range of community and nosocomial infections. The high capacity of this pathogen to acquire resistance drugs makes it necessary to develop therapeutic alternatives, discovering new antibacterial molecules. Acetamides are molecules that have several biological activities. However, there are no reports on the activity of 2-chloro-N-(4-fluoro-3-nitrophenyl)acetamide. Based on this, this study aimed to investigate the in vitro antibacterial activity of this molecule on K. pneumoniae, evaluating whether the presence of the chloro atom improves this effect. Then, analyzing its antibacterial action more thoroughly, as well as its cytotoxic and pharmacokinetic profile, in order to contribute to future studies for the viability of a new antibacterial drug. It was shown that the substance has good potential against K. pneumoniae and the chloro atom is responsible for improving this activity, stabilizing the molecule in the target enzyme at the site. The substance possibly acts on penicillin-binding protein, promoting cell lysis. The analysis of cytotoxicity and mutagenicity shows favorable results for future in vivo toxicological tests to be carried out, with the aim of investigating the potential of this molecule. In addition, the substance showed an excellent pharmacokinetic profile, indicating good parameters for oral use.
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spelling pubmed-75047512020-09-26 Potential of 2-Chloro-N-(4-fluoro-3-nitrophenyl)acetamide Against Klebsiella pneumoniae and In Vitro Toxicity Analysis Cordeiro, Laísa Diniz-Neto, Hermes Figueiredo, Pedro Souza, Helivaldo Sousa, Aleson Andrade-Júnior, Francisco Melo, Thamara Ferreira, Elba Oliveira, Rafael Athayde-Filho, Petrônio Barbosa-Filho, José Oliveira-Filho, Abrahão Lima, Edeltrudes Molecules Article Klebsiella pneumoniae causes a wide range of community and nosocomial infections. The high capacity of this pathogen to acquire resistance drugs makes it necessary to develop therapeutic alternatives, discovering new antibacterial molecules. Acetamides are molecules that have several biological activities. However, there are no reports on the activity of 2-chloro-N-(4-fluoro-3-nitrophenyl)acetamide. Based on this, this study aimed to investigate the in vitro antibacterial activity of this molecule on K. pneumoniae, evaluating whether the presence of the chloro atom improves this effect. Then, analyzing its antibacterial action more thoroughly, as well as its cytotoxic and pharmacokinetic profile, in order to contribute to future studies for the viability of a new antibacterial drug. It was shown that the substance has good potential against K. pneumoniae and the chloro atom is responsible for improving this activity, stabilizing the molecule in the target enzyme at the site. The substance possibly acts on penicillin-binding protein, promoting cell lysis. The analysis of cytotoxicity and mutagenicity shows favorable results for future in vivo toxicological tests to be carried out, with the aim of investigating the potential of this molecule. In addition, the substance showed an excellent pharmacokinetic profile, indicating good parameters for oral use. MDPI 2020-08-31 /pmc/articles/PMC7504751/ /pubmed/32877986 http://dx.doi.org/10.3390/molecules25173959 Text en © 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Cordeiro, Laísa
Diniz-Neto, Hermes
Figueiredo, Pedro
Souza, Helivaldo
Sousa, Aleson
Andrade-Júnior, Francisco
Melo, Thamara
Ferreira, Elba
Oliveira, Rafael
Athayde-Filho, Petrônio
Barbosa-Filho, José
Oliveira-Filho, Abrahão
Lima, Edeltrudes
Potential of 2-Chloro-N-(4-fluoro-3-nitrophenyl)acetamide Against Klebsiella pneumoniae and In Vitro Toxicity Analysis
title Potential of 2-Chloro-N-(4-fluoro-3-nitrophenyl)acetamide Against Klebsiella pneumoniae and In Vitro Toxicity Analysis
title_full Potential of 2-Chloro-N-(4-fluoro-3-nitrophenyl)acetamide Against Klebsiella pneumoniae and In Vitro Toxicity Analysis
title_fullStr Potential of 2-Chloro-N-(4-fluoro-3-nitrophenyl)acetamide Against Klebsiella pneumoniae and In Vitro Toxicity Analysis
title_full_unstemmed Potential of 2-Chloro-N-(4-fluoro-3-nitrophenyl)acetamide Against Klebsiella pneumoniae and In Vitro Toxicity Analysis
title_short Potential of 2-Chloro-N-(4-fluoro-3-nitrophenyl)acetamide Against Klebsiella pneumoniae and In Vitro Toxicity Analysis
title_sort potential of 2-chloro-n-(4-fluoro-3-nitrophenyl)acetamide against klebsiella pneumoniae and in vitro toxicity analysis
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7504751/
https://www.ncbi.nlm.nih.gov/pubmed/32877986
http://dx.doi.org/10.3390/molecules25173959
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