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Abstract <p>In this study, using the plant-derived active compound vanillic acid as the lead structure, a series of novel vanillic acid derivatives containing an 1,2,4-triazole thioether moiety were synthesized and characterized their structures by <sup>1</sup>H, <sup>13</sup>C NMR, and HRMS methods. Then, the in vitro antioxidant and α-glucosidase inhibitory activities of these compounds were evaluated. Bioassay results revealed that the target compounds revealed certain in vitro antioxidant and α-glucosidase inhibitory activities. Among them, compound 3-[4-(benzyloxy)-3-methoxyphenyl]-5-(benzylthio)-4-methyl-4<i>H</i>-1,2,4-triazole exhibited in vitro DPPH scavenging activity at 40 μg/mL and α-glucosidase inhibitory activity at 200 μg/mL, with inhibition rates of 23.4% and 39.4%, respectively, which were even better than those of vanillic acid but lower than those of vitamin C and acarbose. To the best of our knowledge, this is the first report on the synthesis and bioactivity evaluation of this series of novel vanillic acid derivatives containing an 1,2,4-triazole thioether moiety.</p>

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Design, Synthesis, and Bioactivity Evaluation of Novel Vanillic Acid Derivatives Containing an 1,2,4-Triazole Thioether Moiety

  • 期刊论文

  • 发表日期：

    2025年11月1日

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  • Dan Wang,
  • Yongxiang Wu,
  • Wenmin Pan,
  • You Zhang,
  • Xiang Wang,
  • Pei Li

摘要

Abstract

In this study, using the plant-derived active compound vanillic acid as the lead structure, a series of novel vanillic acid derivatives containing an 1,2,4-triazole thioether moiety were synthesized and characterized their structures by 1H, 13C NMR, and HRMS methods. Then, the in vitro antioxidant and α-glucosidase inhibitory activities of these compounds were evaluated. Bioassay results revealed that the target compounds revealed certain in vitro antioxidant and α-glucosidase inhibitory activities. Among them, compound 3-[4-(benzyloxy)-3-methoxyphenyl]-5-(benzylthio)-4-methyl-4H-1,2,4-triazole exhibited in vitro DPPH scavenging activity at 40 μg/mL and α-glucosidase inhibitory activity at 200 μg/mL, with inhibition rates of 23.4% and 39.4%, respectively, which were even better than those of vanillic acid but lower than those of vitamin C and acarbose. To the best of our knowledge, this is the first report on the synthesis and bioactivity evaluation of this series of novel vanillic acid derivatives containing an 1,2,4-triazole thioether moiety.