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<p>Ulcerative Colitis (UC) is a recurrent inflammatory bowel disease with a long and difficult treatment cycle. In this work, a series of new azole derivatives containing ethanolamine moiety have been prepared, and their anti-inflammatory activities were tested. The results indicated that ethanolamine moiety was beneficial for increasing the anti-inflammatory activity of azole derivatives, and most of them showed good inhibition of NO generation. In vivo experiments have shown that <b>7f</b> could reduce the levels of TNF-α and IL-1β cytokines, significantly inhibit the phosphorylation level of p65 NF-κB, and down-regulate the phosphorylation of ERK and JNK on DSS-induced UC model. Therefore, these azole derivatives may be considered as new anti-UC agents by inhibiting NF-κB/MAPK signaling pathways.</p> Graphic Abstract <p></p>

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Exploration of new azole derivatives containing ethanolamine moiety as anti-UC agents by inhibiting NF-κB/MAPK pathways

  • 期刊论文

  • 发表日期：

    2025年11月6日

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  • Ming-Qian Ju,
  • Zheng-Xiao Huang,
  • Qing-Yan Mo,
  • Shuai Liu,
  • Dong-Xue Wang,
  • Yan-Ping Li,
  • Chun-Ping Wan,
  • Ze-Wei Mao

摘要

Ulcerative Colitis (UC) is a recurrent inflammatory bowel disease with a long and difficult treatment cycle. In this work, a series of new azole derivatives containing ethanolamine moiety have been prepared, and their anti-inflammatory activities were tested. The results indicated that ethanolamine moiety was beneficial for increasing the anti-inflammatory activity of azole derivatives, and most of them showed good inhibition of NO generation. In vivo experiments have shown that 7f could reduce the levels of TNF-α and IL-1β cytokines, significantly inhibit the phosphorylation level of p65 NF-κB, and down-regulate the phosphorylation of ERK and JNK on DSS-induced UC model. Therefore, these azole derivatives may be considered as new anti-UC agents by inhibiting NF-κB/MAPK signaling pathways.

Graphic Abstract