Spiropiperidyl rifabutins: expanded in vitro testing against ESKAPE pathogens and select bacterial biofilms
| Autor: | Ana-Belén García, Lindsey N. Shaw, Jessie L Allen, Edward Turos, Bridget G. Budny, María-Paz Cabal, Timothy E. Long |
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| Rok vydání: | 2020 |
| Předmět: |
0301 basic medicine
Staphylococcus aureus Rifabutin Enterococcus faecium 030106 microbiology Human pathogen Microbial Sensitivity Tests medicine.disease_cause 01 natural sciences Article Microbiology Structure-Activity Relationship 03 medical and health sciences Drug Resistance Bacterial Drug Discovery medicine Pharmacology Molecular Structure biology 010405 organic chemistry Biofilm Rifamycin biochemical phenomena metabolism and nutrition biology.organism_classification Rifamycins In vitro Anti-Bacterial Agents 0104 chemical sciences Biofilms Bacteria medicine.drug |
| Zdroj: | J Antibiot (Tokyo) |
| ISSN: | 1881-1469 0021-8820 |
| DOI: | 10.1038/s41429-020-0346-x |
| Popis: | The expanded microbiological evaluation of a series of rifastures, novel spiropiperidyl rifamycin derivatives, against clinically relevant ESKAPE bacteria has identified several analogs with promising in vitro bioactivities against antibiotic-resistant strains of Enterococcus faecium and Staphylococcus aureus. Thirteen of the rifastures displayed minimum inhibitory concentrations (MICs) below 1 μg/ml against the methicillin- and vancomycin-resistant forms of S. aureus and E. faecium (MRSA, VRSA, VRE). Aryl-substituted rifastures 1, 11, and 12 offered the greatest bioactivity, with MICs reaching ≤0.063 μg ml(−1) for these human pathogens. Further analysis indicates that diphenyl rifasture 1 had greater antibiofilm activity against S. aureus and lower cytotoxicity in mammalian HEK cells than rifabutin. |
| Databáze: | OpenAIRE |
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