Cargando…
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...
Autores principales: | , , , , , , , , , , , , |
---|---|
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 |
_version_ | 1783584695842242560 |
---|---|
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. |
format | Online Article Text |
id | pubmed-7504751 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2020 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
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 |
work_keys_str_mv | AT cordeirolaisa potentialof2chloron4fluoro3nitrophenylacetamideagainstklebsiellapneumoniaeandinvitrotoxicityanalysis AT diniznetohermes potentialof2chloron4fluoro3nitrophenylacetamideagainstklebsiellapneumoniaeandinvitrotoxicityanalysis AT figueiredopedro potentialof2chloron4fluoro3nitrophenylacetamideagainstklebsiellapneumoniaeandinvitrotoxicityanalysis AT souzahelivaldo potentialof2chloron4fluoro3nitrophenylacetamideagainstklebsiellapneumoniaeandinvitrotoxicityanalysis AT sousaaleson potentialof2chloron4fluoro3nitrophenylacetamideagainstklebsiellapneumoniaeandinvitrotoxicityanalysis AT andradejuniorfrancisco potentialof2chloron4fluoro3nitrophenylacetamideagainstklebsiellapneumoniaeandinvitrotoxicityanalysis AT melothamara potentialof2chloron4fluoro3nitrophenylacetamideagainstklebsiellapneumoniaeandinvitrotoxicityanalysis AT ferreiraelba potentialof2chloron4fluoro3nitrophenylacetamideagainstklebsiellapneumoniaeandinvitrotoxicityanalysis AT oliveirarafael potentialof2chloron4fluoro3nitrophenylacetamideagainstklebsiellapneumoniaeandinvitrotoxicityanalysis AT athaydefilhopetronio potentialof2chloron4fluoro3nitrophenylacetamideagainstklebsiellapneumoniaeandinvitrotoxicityanalysis AT barbosafilhojose potentialof2chloron4fluoro3nitrophenylacetamideagainstklebsiellapneumoniaeandinvitrotoxicityanalysis AT oliveirafilhoabrahao potentialof2chloron4fluoro3nitrophenylacetamideagainstklebsiellapneumoniaeandinvitrotoxicityanalysis AT limaedeltrudes potentialof2chloron4fluoro3nitrophenylacetamideagainstklebsiellapneumoniaeandinvitrotoxicityanalysis |