Antibacterial and antibiofilm activities of synthetic analogs of 3-alkylpyridine marine alkaloids
| Autor: | Karina Marjorie Silva Herrera, Jaqueline Maria Siqueira Ferreira, Camila de Souza Barbosa, Fernanda Kelen da Silva, Alessandra Mirtes Marques Neves Gonçalves, Gustavo Henrique Ribeiro Viana, Adriana Cristina Soares, William Gustavo Lima |
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| Rok vydání: | 2020 |
| Předmět: |
biology
010405 organic chemistry Viscosaline Klebsiella pneumoniae Chemistry Organic Chemistry Biofilm medicine.disease_cause biology.organism_classification Antimicrobial 01 natural sciences In vitro 0104 chemical sciences Microbiology Clinical Practice 010404 medicinal & biomolecular chemistry Staphylococcus aureus medicine General Pharmacology Toxicology and Pharmaceutics Polymyxin B medicine.drug |
| Zdroj: | Medicinal Chemistry Research. 29:1084-1089 |
| ISSN: | 1554-8120 1054-2523 |
| DOI: | 10.1007/s00044-020-02549-w |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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