Anti-Staphylococcus aureus Methicillin-Resistant (MRSA) Activity of a Novel 3-Chalcogenyl Indole

Laisa Borges Ferreira; Edilma Elayne da Silva; Silvia Adriana Meyer Lentz; Juliano Braun de Azeredo; Antonio Luiz Braga; Michel Mansur Machado; Mario Lettieri Teixeira; Juliana Caierão; Gustavo Pozza Silveira; Andreza Francisco Martins

doi:10.15448/1980-6108.2021.1.41325

Authors

Laisa Borges Ferreira Federal University of Rio Grande do Sul (UFRGS). https://orcid.org/0000-0003-4005-4364
Edilma Elayne da Silva Federal University of Rio Grande do Sul (UFRGS). https://orcid.org/0000-0002-2905-6054
Silvia Adriana Meyer Lentz Federal University of Rio Grande do Sul (UFRGS). https://orcid.org/0000-0002-0118-6797
Juliano Braun de Azeredo Federal University of Rio Grande do Sul (UFRGS). https://orcid.org/0000-0001-6277-0754
Antonio Luiz Braga Federal University of Rio Grande do Sul (UFRGS). https://orcid.org/0000-0001-9903-6764
Michel Mansur Machado Federal University of Rio Grande do Sul (UFRGS). https://orcid.org/0000-0002-7583-9332
Mario Lettieri Teixeira Federal University of Rio Grande do Sul (UFRGS). https://orcid.org/0000-0003-4546-5584
Juliana Caierão Federal University of Rio Grande do Sul (UFRGS). http://orcid.org/0000-0002-8776-8447
Gustavo Pozza Silveira Federal University of Rio Grande do Sul (UFRGS). https://orcid.org/0000-0001-8539-2610
Andreza Francisco Martins Federal University of Rio Grande do Sul (UFRGS). https://orcid.org/0000-0001-6227-1920

DOI:

https://doi.org/10.15448/1980-6108.2021.1.41325

Keywords:

anti-MRSA, chalcogenyl-indoles, new antimicrobials, time-kill, Staphylococcus aureus

Abstract

Objective: the development of new drugs against Methicillin-resistant Staphylococcus aureus is a priority to the World Health Organization. So, the objective of this study was to evaluate the antibacterial activity and toxicity of 5-bromo-3-((4-methoxyphenyl) sulfenyl)-1H-indole (3b) against MRSA.
Methods: minimum inhibitory concentration (MIC) of 3b was determined against S. aureus ATCC 29213 and 43 clinical isolates. The time-kill assay was performed for 9 isolates. Analysis of variance followed by the post hoc Bonferroni test was used for the statistical tests.
Results and conclusions: the MIC50 and MIC90 of 3b were 4 μg.mL-1 and 16 μg.mL-1 respectively. In time-kill assay, the 3b showed bactericidal activity to all evaluated isolates at concentrations of 1xMIC and 2xMIC and the re-growth effect was not observed. About the toxicity tests, 3b has not presented cytotoxicity, mutagenicity, or allergenicity. 3b had particularly good activity against MRSA demonstrating high potential for the development of new antimicrobials products.

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Author Biographies

Laisa Borges Ferreira, Federal University of Rio Grande do Sul (UFRGS).

Master in Agricultural and environmental Microbiology, Institute of Health Sciences, Federal University of Rio Grande do Sul (UFRGS), in Porto Alegre, RS, Brazil. Clinical Research coordinator at Hospital de Clínicas de Porto Alegre, Porto Alegre, RS, Brazil.

Edilma Elayne da Silva, Federal University of Rio Grande do Sul (UFRGS).

Master in Chemistry, Federal University of Pernambuco, RE, Brazil. Doctorate Student in Organic chemistry, Institute of Chemistry (IQ), Federal University of Rio Grande do Sul (UFRGS), in Porto Alegre, RS, Brazil.

Silvia Adriana Meyer Lentz, Federal University of Rio Grande do Sul (UFRGS).

Master in Agricultural and Environmental Microbiology, Institute of Health Sciences, Federal University of Rio Grande do Sul (UFRGS), in Porto Alegre, RS, Brazil. Doctorate student at in Agricultural and Environmental Microbiology, Institute of Health Sciences, Federal University of Rio Grande do Sul (UFRGS), in Porto Alegre, RS, Brazil.

Juliano Braun de Azeredo, Federal University of Rio Grande do Sul (UFRGS).

PhD and Master in Organig Chemistry, Federal University of Santa Catarina (UFSC), in Florianópolis, SC, Brazil. Professor at Organic Chemistry and Pharmacognosy Laboratory, Federal University of Pampa (UNIPAMPA), in Uruguaiana, RS, Brazil.

Antonio Luiz Braga, Federal University of Rio Grande do Sul (UFRGS).

PhD and Master in Organig Chemistry, Federal University of São Paulo (UNIFESP), in São Paulo, SP, Brazil. Professor at Chemistry department, Federal University of Santa Catarina (UFSC), in Florianópolis, SC, Brazil.

Michel Mansur Machado, Federal University of Rio Grande do Sul (UFRGS).

PhD in Biological Science, Federal University of Santa Maria (UFSM), in Santa Maria, RS, Brazil. Master in Pharmaceutical Science, Federal University of Santa Maria (UFSM), in Santa Maria, RS, Brazil. Professor at Clinical Immunology and Toxicology Laboratory, Federal University of Pampa (UNIPAMPA), in Uruguaiana, RS, Brazil.

Mario Lettieri Teixeira, Federal University of Rio Grande do Sul (UFRGS).

PhD and Master in Molecular and Cellular Biology, Federal University of Rio Grande do Sul (UFRGS), in Porto Alegre, RS, Brazil. Professor at Federal Institute of Santa Catarina, in Concórdia, SC, Brazil.

Juliana Caierão, Federal University of Rio Grande do Sul (UFRGS).

PhD in Science, Federal University of Rio de Janeiro (UFRJ), in Rio de Janeiro, RJ, Brazil. Master in Medical Science, Federal University of Health Science of Porto Alegre, in Porto Alegre, RS, Brazil (UFCSPA). Professor at Postgraduate Program in Pharmaceutical Sciences, Federal University of Rio Grande do Sul, in Porto Alegre, RS, Brazil.

Gustavo Pozza Silveira, Federal University of Rio Grande do Sul (UFRGS).

Doctor in Chemistry, Federal University of Santa Catarina (UFSC), in Florianópolis, SC, Brazil. Professor at Federal University of Rio Grande do Sul (UFRGS), in Porto Alegre, RS, Brazil.

Andreza Francisco Martins, Federal University of Rio Grande do Sul (UFRGS).

Doctor in Medical Science, Federal University of Rio Grande do Sul (UFRGS), in Porto Alegre, RS, Brazil. Master in Pharmaceutical Science, Federal University of Rio Grande do Sul (UFRGS), in Porto Alegre, RS, Brazil. Professor at Federal University of Rio Grande do Sul (UFRGS), in Porto Alegre, RS, Brazil.

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