Novel biaryl oxazolidinones: in vitro and in vivo activities with pharmacokinetics in an animal model

Barman, Tarani Kanta; Pandya, Manisha; Mathur, Tarun; Bhadauriya, Tripti; Rao, Madhvi; Khan, Sanaullah; Singhal, Smita; Bhateja, Pragya; Sood, Ruchi; Malhotra, Sunita; Das, Biswajit; Paliwal, Jyoti; Bhatnagar, Pradip K.; Upadhyay, Dilip J.

doi:10.1016/j.ijantimicag.2008.08.025

Cited by 10 publications

(11 citation statements)

References 15 publications

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“…Mouse pulmonary infection with sensitive S. pneumoniae ATCC 6303. Pulmonary infection was established with S. pneumoniae ATCC 6303 as described by Barman et al (26). Briefly, a culture grown overnight was suspended in sterile saline to obtain 1 ϫ 10 8 CFU/ml.…”

Section: Methodsmentioning

confidence: 99%

A Novel Ketolide, RBx 14255, with Activity against Multidrug-Resistant Streptococcus pneumoniae

Raj¹,

Barman²,

Kalia³

et al. 2014

Antimicrob Agents Chemother

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We present here the novel ketolide RBx 14255, a semisynthetic macrolide derivative obtained by the derivatization of clarithromycin, for its in vitro and in vivo activities against sensitive and macrolide-resistant Streptococcus pneumoniae. RBx 14255 showed excellent in vitro activity against macrolide-resistant S. pneumoniae, including an in-house-generated telithromycinresistant strain (S. pneumoniae 3390 NDDR). RBx 14255 also showed potent protein synthesis inhibition against telithromycinresistant S. pneumoniae 3390 NDDR. The binding affinity of RBx 14255 toward ribosomes was found to be more than that for other tested drugs. The in vivo efficacy of RBx 14255 was determined in murine pulmonary infection induced by intranasal inoculation of S. pneumoniae ATCC 6303 and systemic infection with S. pneumoniae 3390 NDDR strains. The 50% effective dose (ED 50 ) of RBx 14255 against S. pneumoniae ATCC 6303 in a murine pulmonary infection model was 3.12 mg/kg of body weight. In addition, RBx 14255 resulted in 100% survival of mice with systemic infection caused by macrolide-resistant S. pneumoniae 3390 NDDR at 100 mg/kg four times daily (QID) and at 50 mg/kg QID. RBx 14255 showed favorable pharmacokinetic properties that were comparable to those of telithromycin.

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Section: Methodsmentioning

confidence: 99%

A Novel Ketolide, RBx 14255, with Activity against Multidrug-Resistant Streptococcus pneumoniae

Raj¹,

Barman²,

Kalia³

et al. 2014

Antimicrob Agents Chemother

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“…Novel biaryl oxazolidinones have been previously demonstrated to have potent activity against Gram-positive bacteria [253]. RBx 11760 is a novel biaryl oxazolidinone compound that was reported by Mathur et al in 2011 as a potential anti-difficile agent [254].…”

Section: Newer Agents For CDImentioning

confidence: 99%

Progress in the Discovery of Treatments for C. difficile Infection: A Clinical and Medicinal Chemistry Review

Tsutsumi¹,

Owusu²,

Hurdle³

et al. 2013

CTMC

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Clostridium difficile is an anaerobic, Gram-positive pathogen that causes C. difficile infection, which results in significant morbidity and mortality. The incidence of C. difficile infection in developed countries has become increasingly high due to the emergence of newer epidemic strains, a growing elderly population, extensive use of broad spectrum antibiotics, and limited therapies for this diarrheal disease. Because treatment options currently available for C. difficile infection have some drawbacks, including cost, promotion of resistance, and selectivity problems, new agents are urgently needed to address these challenges. This review article focuses on two parts: the first part summarizes current clinical treatment strategies and agents under clinical development for C. difficile infection; the second part reviews newly reported anti-difficile agents that have been evaluated or reevaluated in the last five years and are in the early stages of drug discovery and development. Antibiotics are divided into natural product inspired and synthetic small molecule compounds that may have the potential to be more efficacious than currently approved treatments. This includes potency, selectivity, reduced cytotoxicity, and novel modes of action to prevent resistance.

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“…RBx 11760 showed better killing potential at 4ϫ MIC than tedizolid and linezolid at the same concentration against S. pneumoniae 5051. PAE is an important pharmacodynamic parameter that can influence the dosing regimens of an antibiotic (20). In PAE experiments, RBx 11760 showed prolonged PAE against MRSA and MRSE compared to linezolid at the same concentration.…”

Section: Discussionmentioning

confidence: 99%

“…A series of aryl-oxazolidinone compounds was synthesized and checked for antibacterial activity by our group (20,21). RBx 11760 (Fig.…”

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confidence: 99%

In Vitro and In Vivo Activities of a Bi-Aryl Oxazolidinone, RBx 11760, against Gram-Positive Bacteria

Barman

Kumar

Mathur

et al. 2016

Antimicrob Agents Chemother

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Novel biaryl oxazolidinones: in vitro and in vivo activities with pharmacokinetics in an animal model

Cited by 10 publications

References 15 publications

A Novel Ketolide, RBx 14255, with Activity against Multidrug-Resistant Streptococcus pneumoniae

A Novel Ketolide, RBx 14255, with Activity against Multidrug-Resistant Streptococcus pneumoniae

Progress in the Discovery of Treatments for C. difficile Infection: A Clinical and Medicinal Chemistry Review

In Vitro and In Vivo Activities of a Bi-Aryl Oxazolidinone, RBx 11760, against Gram-Positive Bacteria

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