| Autor: |
Filipa, Mota, Ravindra, Jadhav, Camilo A, Ruiz-Bedoya, Alvaro A, Ordonez, Mariah H, Klunk, Joel S, Freundlich, Sanjay K, Jain |
| Rok vydání: |
2020 |
| Předmět: |
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| Zdroj: |
ACS Infect Dis |
| ISSN: |
2373-8227 |
| Popis: |
Oxazolidinones are a novel class of antibacterials with excellent activity against resistant Gram-positive bacteria including strains causing multidrug-resistant tuberculosis (TB). Despite their excellent efficacy, optimal dosing strategies to limit their toxicities are still under development. Here, we developed a novel synthetic strategy for fluorine-18-radiolabeled oxazolidinones. As proof-of-concept, we performed whole-body 18F-linezolid positron emission tomography (PET) in a mouse model of pulmonary TB for noninvasive in situ measurements of time–activity curves in multiple compartments with subsequent confirmation by ex vivo tissue gamma counting. After intravenous injection, (18)F-linezolid rapidly distributed to all organs with excellent penetration into Mycobacterium tuberculosis-infected lungs. Drug biodistribution studies with PET can provide unbiased, in situ drug measurements, which could boost efforts to optimize antibiotic dosing strategies. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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