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<p>Nitroaromatic small molecules are established anti-infectives, including against trypanosomal diseases. Inspired by our previously identified suicide inhibitors of <i>Mycobacterium tuberculosis</i> (<i>Mtb</i>) decaprenylphosphoryl-β-d-ribose 2′-epimerase (DprE1), we report the synthesis and in vitro antitrypanosomal activity of six novel nitroquinoline derivatives (<b>4a-4f</b>), as well as the antitrypanosomal activity of 13 previously described nitroquinolone anti-Mtb compounds, <b>8a-8&#xa0;m</b>. Two compounds exhibited sub-micromolar activity (EC<sub>50</sub> = 0.3–0.5&#xa0;µM), while thirteen compounds exhibited low micromolar activity (EC<sub>50</sub> = 1.1–8.0&#xa0;µM) against <i>Trypanosoma brucei</i>. This study highlights nitroquinolones and nitroquinolines as a source of compounds that exhibit both antitrypanosomal and antitubercular activities.</p> Graphical abstract <p></p>

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Nitroquinolones and nitroquinolines: syntheses and antitrypanosomal activity

  • 期刊论文

  • 发表日期：

    2025年11月21日

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  • Phelelisiwe S. Dube,
  • Karol R. Francisco,
  • Lesetja J. Legoabe,
  • Yujie Uli Sun,
  • Yashpreet Kaur,
  • Tina P. Nguyen,
  • Conor R. Caffrey,
  • Richard M. Beteck

摘要

Nitroaromatic small molecules are established anti-infectives, including against trypanosomal diseases. Inspired by our previously identified suicide inhibitors of Mycobacterium tuberculosis (Mtb) decaprenylphosphoryl-β-d-ribose 2′-epimerase (DprE1), we report the synthesis and in vitro antitrypanosomal activity of six novel nitroquinoline derivatives (4a-4f), as well as the antitrypanosomal activity of 13 previously described nitroquinolone anti-Mtb compounds, 8a-8 m. Two compounds exhibited sub-micromolar activity (EC50 = 0.3–0.5 µM), while thirteen compounds exhibited low micromolar activity (EC50 = 1.1–8.0 µM) against Trypanosoma brucei. This study highlights nitroquinolones and nitroquinolines as a source of compounds that exhibit both antitrypanosomal and antitubercular activities.

Graphical abstract