is a highly pathogenic drug-resistant rapidly growing mycobacterium. In this study, we evaluated the , intracellular, and activities of LCB01-0371, a novel and safe oxazolidinone derivative, for the treatment of infection and compared its resistance to that of other oxazolidinone drugs. LCB01-0371 was effective against several strains and in a macrophage model of infection. In the murine model, a similar efficacy to linezolid was achieved, especially in the lungs. We induced laboratory-generated resistance to LCB01-0371; sequencing analysis revealed mutations in of T424C and G419A and a nucleotide insertion at the 503 position. Furthermore, LCB01-0371 inhibited the growth of amikacin-, cefoxitin-, and clarithromycin-resistant strains. Collectively, our data indicate that LCB01-0371 might represent a promising new class of oxazolidinones with improved safety, which may replace linezolid for the treatment of .
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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5571369 | PMC |
http://dx.doi.org/10.1128/AAC.02752-16 | DOI Listing |
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