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Abstract <p>This study presents the synthesis and optimization of series of 2-(4-((5-bromo-3-formyl-1<i>H</i>-indol-1-yl)methyl)-1<i>H</i>-1,2,3-triazol-1-yl)-<i>N</i>-phenylacetamide derivatives <b>(8a-8t)</b>, synthesized through a multi-step process using a click chemistry approach in a mixed solvent system of <i>tert-</i>butanol, DMF, and water, catalyzed by copper. Optimal reaction conditions provide the highest yield. Subsequent <i>vitro</i> evaluation of 20 synthesized compounds for anti-mycobacterial activity against <i>Mycobacterium tuberculosis</i> revealed that most derivatives were ineffective due to solubility issues. Only a few compounds showed moderate activity, with the reference drug Rifampicin demonstrating significantly higher efficacy. This underscores the need for further optimization of these derivatives to improve their biological activity<i>.</i></p>

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Cu-Mediated Click Chemistry Approach: Synthesis, Characterization, and Anti-Mycobacterial Activity of 2-(4-((5-Bromo-3-formyl-1H-indol-1-yl)methyl)-1H-1,2,3-triazol-1-yl)-N-phenylacetamide Derivatives

  • 期刊论文

  • 发表日期：

    2025年3月1日

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  • Parth Manvar,
  • Dharmesh Katariya,
  • Amita Vyas,
  • Pooja Bhanderi,
  • Ranjan Khunt

摘要

Abstract

This study presents the synthesis and optimization of series of 2-(4-((5-bromo-3-formyl-1H-indol-1-yl)methyl)-1H-1,2,3-triazol-1-yl)-N-phenylacetamide derivatives (8a-8t), synthesized through a multi-step process using a click chemistry approach in a mixed solvent system of tert-butanol, DMF, and water, catalyzed by copper. Optimal reaction conditions provide the highest yield. Subsequent vitro evaluation of 20 synthesized compounds for anti-mycobacterial activity against Mycobacterium tuberculosis revealed that most derivatives were ineffective due to solubility issues. Only a few compounds showed moderate activity, with the reference drug Rifampicin demonstrating significantly higher efficacy. This underscores the need for further optimization of these derivatives to improve their biological activity.