Literature DB >> 23142085

Anti-anaerobic potential of ranbezolid: insight into its mechanism of action against Bacteroides fragilis.

Tarun Mathur1, Vandana Kalia, Tarani Kanta Barman, Smita Singhal, Seema Khan, Dilip J Upadhyay, Ashok Rattan, V Samuel Raj.   

Abstract

This study reports the anti-anaerobic properties of ranbezolid, a new investigational oxazolidinone. A time-kill kinetics study against anaerobes showed that ranbezolid was superior to linezolid and killed the anaerobic pathogens at 4-8h, except for Bacteroides fragilis where killing was observed at 24h. In addition, the time-kill kinetics study showed a concentration-dependent bactericidal potential of ranbezolid against anaerobes. Ranbezolid showed 5.39log(10) reduction and linezolid showed 1.15log(10) reduction in murine disk implant infection with B. fragilis ATCC 25285. Ranbezolid was very potent and showed fast protein synthesis inhibition against B. fragilis, a Gram-negative anaerobe. In addition, non-specific cell wall synthesis inhibition was also observed with ranbezolid. The potent and fast protein synthesis inhibition along with an additional mode of action of cell wall synthesis inhibition could be responsible for the cidal effect of ranbezolid against Gram-negative anaerobes.
Copyright © 2012 Elsevier B.V. and the International Society of Chemotherapy. All rights reserved.

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Year:  2012        PMID: 23142085     DOI: 10.1016/j.ijantimicag.2012.09.013

Source DB:  PubMed          Journal:  Int J Antimicrob Agents        ISSN: 0924-8579            Impact factor:   5.283


  2 in total

1.  (4S)-4-[(R)-Chloro-(4-nitro-phen-yl)meth-yl]-1,3-oxazolidin-2-one.

Authors:  V Gaumet; C Denis; M Madesclaire; V P Zaitsev
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2013-04-24

Review 2.  Progress in the discovery of treatments for C. difficile infection: A clinical and medicinal chemistry review.

Authors:  Lissa S Tsutsumi; Yaw B Owusu; Julian G Hurdle; Dianqing Sun
Journal:  Curr Top Med Chem       Date:  2014       Impact factor: 3.295

  2 in total

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