4.7 Article

Design, Synthesis, and Evaluation of Thiol-Activated Sources of Sulfur Dioxide (SO2) as Antimycobacterial Agents

Journal

JOURNAL OF MEDICINAL CHEMISTRY
Volume 55, Issue 1, Pages 553-557

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/jm201023g

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Funding

  1. IISER Pune
  2. NISER Bhubaneshwar
  3. Department of Science and Technology (DST) India [R/FT/CS-89/2010]
  4. Council for Scientific and Industrial Research (CSIR)

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Here, 2,4-dinitrophenylsulfonamides with tunable cysteine-activated SO2 release profiles with half-lives of SO2 release varying from 2 to 63 min are reported. N-Benzyl-2,4-dinitrobenzenesulfonamide (6), which is prepared in one step from commercial sources, had a potency (MIC = 0.15 mu M) of inhibiting Mycobacterium tuberculosis (Mtb) higher than the clinical agent isoniazid (MIC = 0.37 mu M).

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