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<p>1,2,3-triazoline-containing compounds were prepared starting from sodium saccharin salt reacted with allyl chloride to form N- allyl saccharin (<b>1</b>), then reacted with aromatic azides to give compound (<b>2a-g</b>) were hydrolyzed under strong basic conditions to form the carboxylic acid derivative (<b>3a-g</b>). The compounds were identified using analytical and spectral methods [Fourier transform infrared (FT-IR) and some of them <sup>1</sup>H-NMR, <sup>13</sup>C-NMR] shown in the work. The compounds were tested for their biological and antioxidant activity; some compounds were active and others were not. The recently synthesized fourteen compounds produced positive docking results and suitable binding interactions in molecular docking tests on the target 6ul7(Escherichia coli Dihydrofolate Reductase (DHFR) in complex with a novel inhibitor. Function:Dihydrofolate reductase (DHFR) is an essential enzyme in the folate biosynthesis pathway. It catalyzes the reduction of dihydrofolate to tetrahydrofolate, a critical step in the synthesis of nucleotides and DNA. Due to its importance in cell division, DHFR is a prime target for antimicrobial drugs, such as trimethoprim, which inhibit its activity to disrupt bacterial growth). The current findings show that the recently synthesized compounds have promising Escherichia coli inhibitory efficacy.</p>

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Design, Synthesis, Antibacterial and Antioxidant Evaluation of Novel 1,2,3-Triazoline Derivatives Bearing benzo[d]isothiazol-3(2H)-one 1,1-dioxide Moiety

  • 期刊论文

  • 发表日期：

    2025年7月11日

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  • Hayder Raheem Ali,
  • Ahmed Wahed Naser

摘要

1,2,3-triazoline-containing compounds were prepared starting from sodium saccharin salt reacted with allyl chloride to form N- allyl saccharin (1), then reacted with aromatic azides to give compound (2a-g) were hydrolyzed under strong basic conditions to form the carboxylic acid derivative (3a-g). The compounds were identified using analytical and spectral methods [Fourier transform infrared (FT-IR) and some of them 1H-NMR, 13C-NMR] shown in the work. The compounds were tested for their biological and antioxidant activity; some compounds were active and others were not. The recently synthesized fourteen compounds produced positive docking results and suitable binding interactions in molecular docking tests on the target 6ul7(Escherichia coli Dihydrofolate Reductase (DHFR) in complex with a novel inhibitor. Function:Dihydrofolate reductase (DHFR) is an essential enzyme in the folate biosynthesis pathway. It catalyzes the reduction of dihydrofolate to tetrahydrofolate, a critical step in the synthesis of nucleotides and DNA. Due to its importance in cell division, DHFR is a prime target for antimicrobial drugs, such as trimethoprim, which inhibit its activity to disrupt bacterial growth). The current findings show that the recently synthesized compounds have promising Escherichia coli inhibitory efficacy.