Novel Fluorobenzothiazole as a Dual Inhibitor of Gyrase B and Topoisomerase IV Against Gram-Positive Pathogens

References

• Bozdogan B , EselD , WhitenerC , BrowneFA , AppelbaumPC. Antibacterial susceptibility of a vancomycin-resistant Staphylococcus aureus strain isolated at the Hershey Medical Center. J. Antimicrob. Chemother.52(5), 864–868 (2003).
   PubMed Web of Science ®Google Scholar
• Rice LB . Antimicrobial resistance in gram-positive bacteria. Am. J. Med.119(6 Suppl. 1), S11–S19; discussion S62–S70 (2006).
   PubMed Web of Science ®Google Scholar
• Kujath P , KujathC. Complicated skin, skin structure and soft tissue infections – are we threatened by multi-resistant pathogens?Eur. J. Med. Res.15(12), 544–553 (2010).
   PubMed Web of Science ®Google Scholar
• Kumar M , SaadaouiM , AlKhodor S. Infections and pregnancy: effects on maternal and child health. Front. Cell Infect. Microbiol.12, 873253 (2022).
   PubMed Web of Science ®Google Scholar
• Hardgrib N , WangM , JurikAG , PetersenKK. Life-threatening MRSA sepsis with bilateral pneumonia, osteomyelitis, and septic arthritis of the knee in a previously healthy 13-year-old boy: a case report. Acta Radiol. Open5(10), 2058460116677180 (2016).
   Google Scholar
• Augustine T , KumarM , AlKhodor S , Van PanhuysN. Microbial Dysbiosis tunes the immune response towards allergic disease outcomes. Clin. Rev. Allerg. Immunol. doi:10.1007/s12016-022-08939-9 (2022) ( Epub ahead of print).
   PubMed Web of Science ®Google Scholar
• Kohno S , YamaguchiK , AikawaNet al. Linezolid versus vancomycin for the treatment of infections caused by methicillin-resistant Staphylococcus aureus in Japan. J. Antimicrob. Chemother.60(6), 1361–1369 (2007).
   PubMed Web of Science ®Google Scholar
• Rybak JM , RobertsK. Tedizolid phosphate: a next-generation oxazolidinone. Infect. Dis. Ther.4(1), 1–14 (2015).
   PubMed Web of Science ®Google Scholar
• Silverman JA , MortinLI , VanpraaghAD , LiT , AlderJ. Inhibition of daptomycin by pulmonary surfactant: in vitro modeling and clinical impact. J. Infect. Dis.191(12), 2149–2152 (2005).
   PubMed Web of Science ®Google Scholar
• Azam MA , ThathanJ , JubieS. Dual targeting DNA Gyrase B (GyrB) and Topoisomerse IV (ParE) inhibitors: a review. Bioorg. Chem.62, 41–63 (2015).
   PubMed Web of Science ®Google Scholar
• Mathur T , BarmanTK , KumarMet al. In vitro and in vivo activities of DS-2969b, a novel GyrB inhibitor, against Clostridium difficile. Antimicrob. Agents Chemother.62(4), e02157–17(2018).
   PubMed Web of Science ®Google Scholar
• Barman TK , KumarM , ChairaTet al. Potential of the fluoroketolide RBx 14255 against Streptococcus pneumoniae, Neisseria meningitidis and Haemophilus influenzae in an experimental murine meningitis model. J. Antimicrob. Chemother.74(7), 1962–1970 (2019).
   PubMed Web of Science ®Google Scholar
• Durcik M , TomasicT , ZidarNet al. ATP-competitive DNA gyrase and topoisomerase IV inhibitors as antibacterial agents. Expert Opin. Ther. Pat.29(3), 171–180 (2019).
   PubMed Web of Science ®Google Scholar
• Lu J , PatelS , SharmaNet al. Structures of kibdelomycin bound to Staphylococcus aureus GyrB and ParE showed a novel U-shaped binding mode. ACS Chem. Biol.9(9), 2023–2031 (2014).
   PubMed Web of Science ®Google Scholar
• Stokes NR , Thomaides-BrearsHB , BarkerSet al. Biological evaluation of benzothiazole ethyl urea inhibitors of bacterial type II topoisomerases. Antimicrob. Agents Chemother.57(12), 5977–5986 (2013).
   PubMed Web of Science ®Google Scholar
• Goetschi E , AngehrnP , GmuenderHet al. Cyclothialidine and its congeners: a new class of DNA gyrase inhibitors. Pharmacol. Ther.60(2), 367–380 (1993).
   PubMed Web of Science ®Google Scholar
• Nakada N , ShimadaH , HirataTet al. Biological characterization of cyclothialidine, a new DNA gyrase inhibitor. Antimicrob. Agents Chemother.37(12), 2656–2661 (1993).
   PubMed Web of Science ®Google Scholar
• Basarab GS , HillPJ , GarnerCEet al. Optimization of pyrrolamide topoisomerase II inhibitors toward identification of an antibacterial clinical candidate (AZD5099). J. Med. Chem.57(14), 6060–6082 (2014).
   PubMed Web of Science ®Google Scholar
• Nyerges A , TomasicT , DurcikMet al. Rational design of balanced dual-targeting antibiotics with limited resistance. PLOS Biol.18(10), e3000819 (2020).
   PubMed Web of Science ®Google Scholar
• Gjorgjieva M , TomasicT , BarancokovaMet al. Discovery of benzothiazole scaffold-based DNA Gyrase B inhibitors. J. Med. Chem.59(19), 8941–8954 (2016).
   PubMed Web of Science ®Google Scholar
• Barman TK , KumarM , MathurTet al. In vitro and in vivo activities of DS-2969b, a novel GyrB inhibitor, and its water-soluble prodrug, DS11960558, against methicillin-resistant Staphylococcus aureus. Antimicrob. Agents Chemother.62(6), e02556–17 (2018).
   PubMed Web of Science ®Google Scholar
• Talley AK , ThurstonA , MooreGet al. First-in-human evaluation of the safety, tolerability, and pharmacokinetics of SPR720, a novel oral bacterial DNA gyrase (GyrB) inhibitor for mycobacterial infections. Antimicrob. Agents Chemother.65(11), e0120821 (2021).
   PubMed Web of Science ®Google Scholar
• Vandell AG , InoueS , DennieJet al. Phase 1 study to assess the safety, tolerability, pharmacokinetics, and pharmacodynamics of multiple oral doses of DS-2969b, a novel GyrB inhibitor, in healthy subjects. Antimicrob. Agents Chemother.62(5), e02537–17 (2018).
   PubMed Web of Science ®Google Scholar
• Institute. CaLS . Methods for dilution antimicrobial susceptibility tests for bacteria that grow aerobically. Approved standard M7-A10. Clinical and Laboratory Standards Institute, PA, USA (2015).
   Google Scholar
• Kim SH , ParkC , ChunHSet al. Pilot screening to determine antimicrobial synergies in a multidrug-resistant bacterial strain library. Microb. Drug Resist.22(5), 372–378 (2016).
   PubMed Web of Science ®Google Scholar
• Kumar A , KhanIA , KoulSet al. Novel structural analogues of piperine as inhibitors of the NorA efflux pump of Staphylococcus aureus. J. Antimicrob Chemother.61(6), 1270–1276 (2008).
   PubMed Web of Science ®Google Scholar
• Odds FC . Synergy, antagonism, and what the chequerboard puts between them. J. Antimicrob. Chemother.52(1), 1 (2003).
   PubMed Web of Science ®Google Scholar
• Sharma S , KumarM , SharmaS , NargotraA , KoulS , KhanIA. Piperine as an inhibitor of Rv1258c, a putative multidrug efflux pump of Mycobacterium tuberculosis. J. Antimicrob. Chemother.65(8), 1694–1701 (2010).
   PubMed Web of Science ®Google Scholar
• Barman TK , KumarM , MathurTet al. In vitro and in vivo activities of a Bi-Aryl oxazolidinone, RBx 11760, against Gram-positive bacteria. Antimicrob. Agents Chemother.60(12), 7134–7145 (2016).
   PubMed Web of Science ®Google Scholar
• Kumar M , MathurT , BarmanTKet al. In vitro and in vivo activities of the novel ketolide RBx 14255 against Clostridium difficile. Antimicrob. Agents Chemother.56(11), 5986–5989 (2012).
   PubMed Web of Science ®Google Scholar
• Kumar M , RaoM , PurnapatreKPet al. DS86760016, a leucyl-tRNA synthetase inhibitor with activity against Pseudomonas aeruginosa. Antimicrob.Agents Chemother.63(4), e02122–18 (2019).
   PubMed Web of Science ®Google Scholar
• Barman TK , RaoM , BhatiAet al. Non invasive real-time monitoring of bacterial infection & therapeutic effect of anti-microbials in five mouse models. Indian J. Med. Res.134(5), 688–695 (2011).
   PubMedGoogle Scholar
• Rao MB , TarunK , KumarM , MathurT , ShuklaG , BhatiA , KishoreK , ChairaT , PandyaM , UpadhyayDJ. Efficacy of linezolid against Staphylococcus aureus in different rodent skin and soft tissue infections models. Microbiol. Res.2(1), e3 (2011).
   Google Scholar
• Kumar M , MathurT , BarmanTKet al. Novel FtsZ inhibitor with potent activity against Staphylococcus aureus. J. Antimicrob. Chemother.76(11), 2867–2874 (2021).
   PubMed Web of Science ®Google Scholar
• Kumar M , RaoM , MathurTet al. Azithromycin exhibits activity against Pseudomonas aeruginosa in chronic rat lung infection model. Front. Microbiol.12, 603151 (2021).
   PubMedGoogle Scholar
• Bax BD , ChanPF , EgglestonDSet al. Type IIA topoisomerase inhibition by a new class of antibacterial agents. Nature466(7309), 935–940 (2010).
   PubMed Web of Science ®Google Scholar
• Gade ND , QaziMS. Fluoroquinolone therapy in Staphylococcus aureus infections: where do we stand?J. Lab. Physicians5(2), 109–112 (2013).
   PubMedGoogle Scholar
• De Kraker ME , StewardsonAJ , HarbarthS. Will 10 million people die a year due to antimicrobial resistance by 2050?PLOS Med.13(11), e1002184 (2016).
   PubMed Web of Science ®Google Scholar
• Jones RN , FritscheTR , SaderHS , RossJE. LEADER surveillance program results for 2006: an activity and spectrum analysis of linezolid using clinical isolates from the United States (50 medical centers). Diagn. Microbiol. Infect. Dis.59(3), 309–317 (2007).
   PubMed Web of Science ®Google Scholar
• Schwameis R , Erdogan-YildirimZ , ManafiM , ZeitlingerMA , StrommerS , SauermannR. Effect of pulmonary surfactant on antimicrobial activity in vitro. Antimicrob. Agents Chemother.57(10), 5151–5154 (2013).
   PubMed Web of Science ®Google Scholar
• Martinez MN , PapichMG , DrusanoGL. Dosing regimen matters: the importance of early intervention and rapid attainment of the pharmacokinetic/pharmacodynamic target. Antimicrob. Agents Chemother.56(6), 2795–2805 (2012).
   PubMed Web of Science ®Google Scholar
• Kumar M , MathurT , JoshiV , UpadhyayDJ , InoueSI , MasudaN. Effect of DS-2969b, a novel GyrB inhibitor, on rat and monkey intestinal microbiota. Anaerobe51, 120–123 (2018).
   PubMed Web of Science ®Google Scholar