The Derivative Difluoroboranyl-Fluoroquinolone “7a” Generates Effective Inhibition Against the <i>S. aureus</i> Strain in a Murine Model of Acute Pneumonia
During the last decades, most bacterial strains have become increasingly resistant to antibiotics. This led the WHO to declare a global emergency in 2017 and urge the development of new active compounds. Some families of antibiotics still show high antibacterial efficacy, as is the case of fluoroqui...
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| Main Authors: | , , , , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2025-02-01
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| Series: | Current Issues in Molecular Biology |
| Subjects: | |
| Online Access: | https://www.mdpi.com/1467-3045/47/2/110 |
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| Summary: | During the last decades, most bacterial strains have become increasingly resistant to antibiotics. This led the WHO to declare a global emergency in 2017 and urge the development of new active compounds. Some families of antibiotics still show high antibacterial efficacy, as is the case of fluoroquinolones, which have a broad spectrum of action. For this reason, our research group derived several compounds from fluoroquinolones, selecting a compound with good antibacterial activity for further evaluations, a difluoroboranil-fluoroquinolone complex labeled <b>7a</b>. Antibacterial activity was evaluated using the Kirby–Bauer method against <i>S. aureus</i> (clinical isolate HGZ2201#ID). The MIC and MBC were obtained by macrodilutions and reseeding. In vivo antimicrobial activity was evaluated in a Balb/c mouse model infected intratracheally with <i>S. aureus</i> and subsequently treated with ciprofloxacin or <b>7a</b> (80 mg/kg/day) for five days. A mean of 8.55 ± 0.395 cm<sup>2</sup> inhibition area was observed using <b>7a</b>, while ciprofloxacin generated a mean inhibition of 7.86 ± 0.231 cm<sup>2</sup>. Compound <b>7a</b> showed a MIC and MBC of 0.25 μg/mL. This reduced the generation of pneumonic lung tissue to 5.83%, while the untreated infected group generated 60.51% of pneumonic tissue. Compound <b>7a</b> proved to be an antimicrobial agent capable of inhibiting the in vitro development of <i>S. aureus</i>. Furthermore, <b>7a</b> showed effectiveness in decreasing the progression of acute pneumonia induced by <i>S. aureus</i> in a murine model. |
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| ISSN: | 1467-3037 1467-3045 |