| Autor: |
Barman, Tarani K, Kumar, Manoj, Chaira, Tridib, Singhal, Smita, Mathur, Tarun, Kalia, Vandana, Gangadharan, Ramkumar, Rao, Madhvi, Pandya, Manisha, Bhateja, Pragya, Sood, Ruchi, Upadhyay, Dilip J, Varughese, Shibu, Yadav, Ajay, Sharma, Lalima, Ramadass, Venkataramanan, Kumar, Naresh, Sattigeri, Jitendra, Bhatnagar, Pradip K, Raj, V Samuel |
| Zdroj: |
Future Microbiology; July 2023, Vol. 18 Issue: 10 p625-638, 14p |
| Abstrakt: |
Aim:The development of a novel inhibitor targeting gyrase B and topoisomerase IV offers an opportunity to combat multidrug resistance. Methods:We investigated the activity of RBx 10080758 against Gram-positive bacteria in vitroand in vivo. Results:RBx 10080758 showed a potent 50% inhibitory concentration of 0.13 μM and 0.25 μM against gyrase B and topoisomerase IV, respectively, and exhibited strong whole-cell in vitroactivity with MIC ranges of 0.015–0.06 and 0.015–0.03 μg/ml against Staphylococcus aureusand Streptococcus pneumoniae, respectively. In a rat thigh infection model with methicillin-resistant S. aureus, RBx 10080758 at 45 mg/kg exhibited a >3 log10CFU reduction in thigh muscles. Conclusion:RBx 10080758 displayed potent activity against multiple multidrug-resistant Gram-positive bacteria with a dual-targeting mechanism of action. |
| Databáze: |
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