Scholarlink

<p>The functional modification of isoniazid has always been a hotspot in the drug development. In this paper, we have described ultrasound-assisted and [DIPEA][OAc-mediated synthesis of isoniazid based 1,2,3-triazole derivatives via click chemistry approach in excellent yields (upto 95%) and short reaction time (30&#xa0;min). The synthesized derivatives were evaluated for their in vitro antitubercular activity against the <i>Mycobacterium tuberculosis</i> H37Rv strain. Notably, the compound <b>12i</b> exhibited remarkable activity with lower MIC value 1.56&#xa0;µg/mL. All the synthesised compounds were screened for their antioxidant potential and showed comparable IC₅₀ values ranging from 10.01 ± 0.21 to 15.04 ± 0.01&#xa0;µg/mL with the the standard, ascorbic acid. Molecular docking study revealed strong and specific binding interactions with the active site of the <i>Mycobacterial</i> InhA enzyme, in good correlation with experimental data. These results highlight the therapeutic potential of this isoniazid based 1,2,3-triazole derivatives as promising dual-function therapeutic candidates combining direct antitubercular effects with oxidative stress modulation.</p> Graphical abstract <p></p>

错误：搜索内容不能为空，请输入英文关键词
错误：关键词超出字数限制，请精简
高级检索

[DIPEA][OAc]-Mediated and Ultrasound-Assisted Synthesis of Isoniazid Based 1,2,3-Triazoles as Antitubercular and Antioxidant Agents

  • 期刊论文

  • 发表日期：

    2026年1月22日

查看全文
  • Madiha M. Siddiqui,
  • Amol A. Nagargoje,
  • Mubarak H. Shaikh,
  • Dipti D. More,
  • Rashiqua A. Siddiqui,
  • Dharmarajan Sriram,
  • Vijay M. Khedkar,
  • Bapurao B. Shingate

摘要

The functional modification of isoniazid has always been a hotspot in the drug development. In this paper, we have described ultrasound-assisted and [DIPEA][OAc-mediated synthesis of isoniazid based 1,2,3-triazole derivatives via click chemistry approach in excellent yields (upto 95%) and short reaction time (30 min). The synthesized derivatives were evaluated for their in vitro antitubercular activity against the Mycobacterium tuberculosis H37Rv strain. Notably, the compound 12i exhibited remarkable activity with lower MIC value 1.56 µg/mL. All the synthesised compounds were screened for their antioxidant potential and showed comparable IC₅₀ values ranging from 10.01 ± 0.21 to 15.04 ± 0.01 µg/mL with the the standard, ascorbic acid. Molecular docking study revealed strong and specific binding interactions with the active site of the Mycobacterial InhA enzyme, in good correlation with experimental data. These results highlight the therapeutic potential of this isoniazid based 1,2,3-triazole derivatives as promising dual-function therapeutic candidates combining direct antitubercular effects with oxidative stress modulation.

Graphical abstract