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Novel fluorobenzothiazole as a dual inhibitor of gyrase B and topoisomerase IV against Gram-positive pathogens - Supplementary figure 2S

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posted on 2023-08-04, 14:49 authored by Tarani K Barman, Manoj KumarManoj Kumar, Tridib Chaira, Smita Singhal, Tarun Mathur, Vandana Kalia, Ramkumar Gangadharan, Madhvi Rao, Manisha Pandya, Pragya Bhateja, Ruchi Sood, Dilip J Upadhyay, Shibu Varughese, Ajay Yadav, Lalima Sharma, Venkataramanan Ramadass, Naresh Kumar, Jitendra Sattigeri, Pradip K Bhatnagar, V Samuel Raj

  

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 Grampositive bacteria in vitro and 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 wholecell in vitro activity with MIC ranges of 0.015–0.06 and 0.015–0.03 μg/ml against Staphylococcus aureus and Streptococcus pneumoniae, respectively. In a rat thigh infection model with methicillin-resistant S. aureus, RBx 10080758 at 45 mg/kg exhibited a >3 log10 CFU reduction in thigh muscles. Conclusion: RBx 10080758 displayed potent activity against multiple multidrug-resistant Gram-positive bacteria with a dual-targeting mechanism of action.  

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