Design, development of new synthetic methodology, and biological evaluation of substituted quinolines as new anti-tubercular leads

Nov 15, 2016Bioorganic & medicinal chemistry letters

Creating and testing new modified quinoline compounds as potential tuberculosis treatments

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Abstract

Among forty-two tested quinoline-based compounds, twenty-three exhibited significant anti-tubercular activity against Mycobacterium tuberculosis.

  • Compounds 3b and 3c showed excellent anti-TB activity with minimum inhibitory concentrations (MIC) of 0.2 and 0.39μg/mL, respectively.
  • These two compounds were found to be more potent than the standard anti-TB drugs currently in clinical use.
  • All active compounds with MIC values ≤6.25μg/mL demonstrated low toxicity against Human Embryonic Kidney 293T cell lines.
  • The findings indicate that these synthesized quinoline derivatives may serve as promising candidates for new TB treatments.

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