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Assay Development for High-Throughput Drug Screening Against Mycobacteria
Published on: October 25, 2024
In vitro and in vivo antibacterial evaluation of DRF 8417, a new oxazolidinone
K Sreenivas1, P V S Amarnath, A Mallik
1Anti-infective Group, Discovery Research, Dr Reddy's Laboratories Ltd, Miyapur, Hyderabad 500 049, India. sreenivaskandepu@drreddys.com
Objectives And Methods:
DRF 8417, a novel oxazolidinone, has been evaluated against Gram-positive and fastidious Gram-negative bacteria. In vitro activity of DRF 8417 was determined by broth microdilution method and in vivo efficacy studies were carried out in different murine systemic infection models.
Results:
DRF 8417 exhibited potent activity against Gram-positive pathogens with MIC(50) and MIC(90) values ranging from 0.06 to 1 mg/L. MICs against Haemophilus influenzae and Moraxella catarrhalis were one to two dilutions lower than those of linezolid. The in vivo efficacy, by oral route, in different susceptible and resistant Gram-positive systemic bacterial infection models ranged from 2.0 to 2.9 mg/kg.
Conclusions:
These studies displayed the excellent in vitro and in vivo activity of DRF 8417 against Gram-positive pathogens and lower MICs when compared with linezolid against H. influenzae and M. catarrhalis.
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