Abstract
BackgroundDue to the emergency of multidrug-resistant strains of Mycobacterium tuberculosis, is necessary the evaluation of new compounds.FindingsTedizolid, a novel oxazolidinone, and ACH-702, a new isothiazoloquinolone, were tested against M. tuberculosis infected THP-1 macrophages. These two compounds significantly decreased the number of intracellular mycobacteria at 0.25X, 1X, 4X and 16X the MIC value. The drugs were tested either in nanoparticules or in free solution.ConclusionTedizolid and ACH-702 have a good intracellular killing activity comparable to that of rifampin or moxifloxacin.
Highlights
Due to the emergency of multidrug-resistant strains of Mycobacterium tuberculosis, is necessary the evaluation of new compounds
Broth microdilution assay Tedizolid Phosphate was donated by Sung-Hak Choi from Dong-A Pharmaceutical Company, Ltd., Yongin, Korea, while ACH-702 was obtained from Achillion Pharmaceuticals, Inc., New Haven
Stock solutions of 1 mg/ml for moxifloxacin and tedizolid were dissolved in water, ACH-702 was dissolved in dimethyl sulfoxide and rifampin was dissolved in 95% ethanol
Summary
Due to the emergency of multidrug-resistant strains of Mycobacterium tuberculosis, is necessary the evaluation of new compounds. Findings: Tedizolid, a novel oxazolidinone, and ACH-702, a new isothiazoloquinolone, were tested against M. tuberculosis infected THP-1 macrophages. These two compounds significantly decreased the number of intracellular mycobacteria at 0.25X, 1X, 4X and 16X the MIC value. Emergence of multidrug resistant TB strains (MDR), defined as those resistant to at least rifampin and isoniazid, has been a public health threat around the world. It is estimated that about 9% of MDRTB cases had XDR-TB [1] Given this increase in global resistance, new compounds or new therapeutic schemes are urgently needed
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