Ethionamide activation and sensitivity in multidrug-resistant Mycobacterium tuberculosis.

  title={Ethionamide activation and sensitivity in multidrug-resistant Mycobacterium tuberculosis.},
  author={Andrea E Debarber and K Mdluli and Marlein E. Bosman and L G Bekker and Clifton E Barry},
  journal={Proceedings of the National Academy of Sciences of the United States of America},
  volume={97 17},
Ethionamide (ETA) is an important component of second-line therapy for the treatment of multidrug-resistant tuberculosis. Synthesis of radiolabeled ETA and an examination of drug metabolites formed by whole cells of Mycobacterium tuberculosis (MTb) have allowed us to demonstrate that ETA is activated by S-oxidation before interacting with its cellular target. ETA is metabolized by MTb to a 4-pyridylmethanol product remarkably similar in structure to that formed by the activation of isoniazid by… CONTINUE READING
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