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<p>Isoxazole-containing compounds showed an array of biological activities relevant to pulmonary tuberculosis. A series of pyrrolopyrimidine and indole derivatives containing isoxazole rings were constructed and synthesized by employing substituted isoxazole, pyrrolopyrimidine and indole derivatives as raw materials under the optimal reaction condition. On the basis of confirming the structure of the synthesized compounds, their antibacterial activity against <i>Mycobacteria smegmatis</i> in vitro was evaluated using rifampin as a positive control. Two compounds showed excellent anti-mycobacterium activity, and their minimum inhibitory concentrations were respectively 10.67 ± 3.77&#xa0;μg/mL and 8.00&#xa0;μg/mL, which suggested that they can be regarded as candidates for development of anti-tuberculosis drugs.</p> Graphical abstract <p></p>

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Effective synthesis and anti-mycobacteriuml activity of isoxazole-substituted pyrrolopyrimidine and isoxazole-substituted indole derivatives

  • 期刊论文

  • 发表日期：

    2025年4月5日

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  • Yafei Xue,
  • Yongchang Bi,
  • Jingjun Wang,
  • Guangyuan Zhu,
  • Mingyue Chen,
  • Xingyu Bian,
  • Yumin Zhang,
  • Qiang Gu

摘要

Isoxazole-containing compounds showed an array of biological activities relevant to pulmonary tuberculosis. A series of pyrrolopyrimidine and indole derivatives containing isoxazole rings were constructed and synthesized by employing substituted isoxazole, pyrrolopyrimidine and indole derivatives as raw materials under the optimal reaction condition. On the basis of confirming the structure of the synthesized compounds, their antibacterial activity against Mycobacteria smegmatis in vitro was evaluated using rifampin as a positive control. Two compounds showed excellent anti-mycobacterium activity, and their minimum inhibitory concentrations were respectively 10.67 ± 3.77 μg/mL and 8.00 μg/mL, which suggested that they can be regarded as candidates for development of anti-tuberculosis drugs.

Graphical abstract