Apesar de ser parte da microbiota humana normal, Staphylococcus aureus é um dos principais microrganismos patogênicos para o homem, causando desde infecções simples à potencialmente fatais. S. aureus é capaz de desenvolver fatores de resistência aos antimicrobianos, sendo motivo constante de preocupação e um grave problema de saúde pública. Este estudo analisou a prevalência de S. aureus em hospitais do Brasil, bem como seus perfis de resistência aos antimicrobianos, contribuindo para atualização dos profissionais de saúde. Para isso, foi realizada uma revisão integrativa de literatura nas bases de dados PubMed, SciELO, Science Direct e Google Acadêmico, no período entre 2011 e 2021, com as seguintes palavras-chave: Staphylococcus aureus, MRSA, infecção, hospitais do Brasil e resistência, nos idiomas inglês, espanhol e português. Inicialmente foram selecionados 85 artigos, dos quais 35 foram utilizados para construção das tabelas de síntese. A prevalência de S. aureus em amostras de pacientes, profissionais de saúde e superfícies hospitalares, associada aos altos índices de resistência à oxacilina, foi observada na maioria dos artigos analisados. Deste modo, é necessária uma vigilância contínua de S. aureus, bem como alertar os profissionais para a possibilidade de serem portadores desta bactéria, ressaltando a importância da adesão às medidas de prevenção e de controle epidemiológico desse microrganismo.
Aims Antimicrobial resistance is one of the highest priorities in global public health with Staphylococcus aureus among the most important microorganisms due to its rapidly evolving antimicrobial resistance. Despite all the efforts of antimicrobial stewardship, research and development of new antimicrobials are still imperative. The thiazolidine ring is considered a privileged structure for the development of new antimicrobials. This study aimed to compare the antibacterial effects of two analogue series of thiazolidine‐2,4‐dione and 4‐thioxo‐thiazolidin‐2‐one against multidrug‐resistant Staph. aureus clinical isolates. Methods and Results The derivatives 1a, 2a and 2b exhibited MIC between 1–32 μg ml−1, with time‐to‐kill curves showing a bactericidal effect up to 24 h. In the antibiofilm assay, the most active derivatives were able to inhibit about 90% of biofilm formation. The 4‐thioxo‐thiazolidine‐2‐one derivatives were more active against planktonic cells, while the thiazolidine‐2,4‐dione derivatives were able to disrupt about 50% of the preformed biofilm. In the in vivo infection model using Caenorhabditis elegans as a host, the derivatives 1a, 2a and 2b increased nematode survival with a concentration‐dependent effect. Exposure of Staph. aureus to the derivatives 2a and 2b induced surface changes and decrease cell size. None of the derivatives was cytotoxic for human peripheral blood mononuclear cells (PBMC) but showed moderate cytotoxicity for L929 fibroblasts. Conclusion The 5‐(3,4‐dichlorobenzylidene)‐4‐thioxothiazolidin‐2‐one (2b) was the most active derivative against Staph. aureus and showed higher selective indices. Significance and Impact of the Study 4‐thioxo‐thiazolidin‐2‐one is a promising scaffold for the research and development of new antimicrobial drugs against multidrug‐resistant Staph. aureus.
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