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Antibacterial and antibiofilm activities of synthetic analogs of 3-alkylpyridine marine alkaloids

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Abstract

Nowadays, the emergence of superbugs is one of the most serious public health problems. Strains of Staphylococcus aureus and Klebsiella pneumoniae, resistant to many antimicrobials available in clinical practice, have become increasingly common. The development of new drugs for the treatment of infections caused by these pathogens is necessary and urgent. A series of 11 analogs of marine 3-alkylpyridine alkaloids was evaluated in vitro for its antibacterial potential. Compound 6, a synthetic analog of viscosaline, exhibited significant activity against S. aureus, including an MRSA strain (MIC = 2 µg/mL). Additionally, it exhibited a 25% reduction in mature biofilm and a good selectivity index (SI > 16). None of the compounds exhibited activity against K. pneumoniae, but analog 6 was able to act in planktonic cells in the presence of polymyxin B at sub-inhibitory concentration. Compound 6 has promising anti-staphylococcal activity and future assays are encouraged to investigate their therapeutic potential.

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Acknowledgements

We would like to thank Universidade Federal de São João del-Rei, Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq), Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES), Fundação de Amparo à Pesquisa do estado de Minas Gerais (FAPEMIG) for the support, Agnes Marie Sá Figueiredo (UFRJ, Rio de Janeiro, Brazil) for the supply of the MRSA USA 300 strain, and Camyla Alves Leonel (UFSJ, Minas Gerais, Brazil) for performing the cytotoxicity assay.

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Authors and Affiliations

  1. Laboratório de Microbiologia Médica, Universidade Federal de São João del-Rei (UFSJ), Campus Centro Oeste Dona Lindu, Divinópolis, Minas Gerais, Brazil

    Karina M. S. Herrera, Fernanda K. da Silva, William G. de Lima & Jaqueline M. S. Ferreira

  2. Laboratório de Síntese Orgânica, Universidade Federal de São João del-Rei (UFSJ), Campus Centro Oeste Dona Lindu, Divinópolis, Minas Gerais, Brazil

    Camila de S. Barbosa, Alessandra M. M. N. Gonçalves & Gustavo H. R. Viana

  3. Laboratório de Farmacologia, Universidade Federal de São João del-Rei (UFSJ), Campus Centro Oeste Dona Lindu, Divinópolis, Minas Gerais, Brazil

    Adriana C. Soares

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  1. Karina M. S. Herrera
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  2. Fernanda K. da Silva
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Correspondence to Karina M. S. Herrera.

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Herrera, K.M.S., da Silva, F.K., de Lima, W.G. et al. Antibacterial and antibiofilm activities of synthetic analogs of 3-alkylpyridine marine alkaloids. Med Chem Res 29, 1084–1089 (2020). https://doi.org/10.1007/s00044-020-02549-w

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