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Abstract <p>A broad approach for the synthesis of fused [1,2,3]triazolo[1′,5′:2,3]isothiazolo[4,5-<i>d</i>]pyrimidines from 2-chloropyrimidine-5-sulfonyl chloride, NaN<sub>3</sub>, and several iodoalkynes was established <i>via</i> microwave-assisted one-pot Cu-catalyzed cycloaddition followed by C–C bong coupling reaction under PEG-400 medium. In vitro antibacterial efficacy of newly synthesized compounds against three Gram-positive bacterial strains such as <i>Bacillus subtilis</i>, <i>Staphylococcus aureus</i>, and <i>Staphylococcus epidermidis</i>. Two compounds were more active against two bacterial strains: <i>B. subtilis</i> and <i>S. aureus</i>. Furthermore, these two compounds have demonstrated significant biofilm action against <i>S. aureus</i>. We performed <i>in silico</i> investigations to evaluate the molecular interactions of more powerful drugs with TLR<sub>4</sub> proteins (PDB: 3FXI, 3VQ1, 3RG1). Our findings showed that the studied potent chemicals had higher binding energies to human, mouse, and bovine TLR4 proteins than dicloxacillin.</p>

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Synthesis, Antibacterial, Antibiofilm, and TLR4 Inhibitory Activity of Novel Fused [1,2,3]Triazolo[1′,5′:2,3]isothiazolo[4,5-d]pyrimidines

  • 期刊论文

  • 发表日期：

    2025年11月1日

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  • S. S. Ardhapure,
  • N. B. Chavhan,
  • S. L. Shinde,
  • S. B. Sirsat

摘要

Abstract

A broad approach for the synthesis of fused [1,2,3]triazolo[1′,5′:2,3]isothiazolo[4,5-d]pyrimidines from 2-chloropyrimidine-5-sulfonyl chloride, NaN3, and several iodoalkynes was established via microwave-assisted one-pot Cu-catalyzed cycloaddition followed by C–C bong coupling reaction under PEG-400 medium. In vitro antibacterial efficacy of newly synthesized compounds against three Gram-positive bacterial strains such as Bacillus subtilis, Staphylococcus aureus, and Staphylococcus epidermidis. Two compounds were more active against two bacterial strains: B. subtilis and S. aureus. Furthermore, these two compounds have demonstrated significant biofilm action against S. aureus. We performed in silico investigations to evaluate the molecular interactions of more powerful drugs with TLR4 proteins (PDB: 3FXI, 3VQ1, 3RG1). Our findings showed that the studied potent chemicals had higher binding energies to human, mouse, and bovine TLR4 proteins than dicloxacillin.