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Abstract <p>A new homologous class of 1,2,3-triazole–purine hybrids—<i>N</i>-aryl-2-{4-[(2,6-dichloro-9<i>H</i>-purin-9-yl)methyl]-1,2,3-triazol-1-yl)acetamides—was synthesized via copper(I)-catalyzed azide–alkyne cycloaddition (CuAAC) of <i>N</i>-aryl-2-azidoacetamide derivatives to 2,6-dichloro-9-(prop-2-yn-1-yl)-9<i>H</i>-purine. The structure of the synthesized compounds was confirmed by IR and NMR (<sup>1</sup>H and <sup>13</sup>C) spectroscopy and mass spectrometry. The products were screened for antimicrobial activity against Gram-positive (<i>Bacillus subtilis</i>, <i>Staphylococcus aureus</i>, and <i>Staphylococcus epidermidis</i>) and Gram-negative (<i>Escherichia coli</i>, <i>Pseudomonas aeruginosa</i>) bacteria, as well as <i>Aspergillus niger</i>, <i>Candida albicans</i>, and <i>Aspergillus flavus</i> fungi. Two of them (Ar = 4-nitrophenyl and 4-ethylphenyl) exhibited superior antibacterial and antifungal properties, demonstrating minimum inhibitory concentrations (MICs) as low as 3.125 µg/mL against <i>B. subtilis</i> and <i>A. niger</i>, respectively. These results suggest that purine-triazole hybrids show promise as potential antibacterial agents.</p>

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Synthesis and Antimicrobial Evaluation of Novel Homologous Series of N-Aryl-2-{4-[(2,6-dichloro-9H-purin-9-yl)methyl]-1H-1,2,3-triazol-1-yl}acetamides

  • 期刊论文

  • 发表日期：

    2026年1月1日

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  • Hina K. Tilavat,
  • Heta B. Vasveliya,
  • Amita K. Vyas,
  • Kalpesh R. Kholiya,
  • Kavan Andhariya,
  • Ramesh Kothari,
  • Jatin Upadhyay

摘要

Abstract

A new homologous class of 1,2,3-triazole–purine hybrids—N-aryl-2-{4-[(2,6-dichloro-9H-purin-9-yl)methyl]-1,2,3-triazol-1-yl)acetamides—was synthesized via copper(I)-catalyzed azide–alkyne cycloaddition (CuAAC) of N-aryl-2-azidoacetamide derivatives to 2,6-dichloro-9-(prop-2-yn-1-yl)-9H-purine. The structure of the synthesized compounds was confirmed by IR and NMR (1H and 13C) spectroscopy and mass spectrometry. The products were screened for antimicrobial activity against Gram-positive (Bacillus subtilis, Staphylococcus aureus, and Staphylococcus epidermidis) and Gram-negative (Escherichia coli, Pseudomonas aeruginosa) bacteria, as well as Aspergillus niger, Candida albicans, and Aspergillus flavus fungi. Two of them (Ar = 4-nitrophenyl and 4-ethylphenyl) exhibited superior antibacterial and antifungal properties, demonstrating minimum inhibitory concentrations (MICs) as low as 3.125 µg/mL against B. subtilis and A. niger, respectively. These results suggest that purine-triazole hybrids show promise as potential antibacterial agents.