2. Academic Validation
  3. Synthesis, anti-allergic rhinitis evaluation and mechanism investigation of novel 1,2,4-triazole-enamides as CB1 R antagonist

Synthesis, anti-allergic rhinitis evaluation and mechanism investigation of novel 1,2,4-triazole-enamides as CB1 R antagonist

  • Eur J Med Chem. 2025 Feb 27:289:117461. doi: 10.1016/j.ejmech.2025.117461.
Lu Wang 1,  Yan Geng 2,  Lifang Liu 3,  Jun Wang 2,  Jiaxin Chen 2,  Yunying Li 1,  Jingbo Wang 4,  Liyan Song 5,  Kexin Sun 2,  Yajie Yan 1,  Shiqing Zhou 1,  Dan Tian 2,  Ran Lin 6,  Hongliang Yao 7
Affiliations

Affiliations

  • 1 The Second Clinical College of Guangzhou University of Chinese Medicine, Otorhinolaryngology Head and Neck Department, The Second Affiliated Hospital of Guangzhou University of Chinese Medicine, Yuexiu District, Dade Road111, Guangzhou, Guangdong, China.
  • 2 Guangdong Key Laboratory of Animal Conservation and Resource Utilization, Guangdong Public Laboratory of Wild Animal Conservation and Utilization, Institute of Zoology, Guangdong Academy of Sciences, Guangzhou, Guangdong, China.
  • 3 Department of Biopharmaceutical Sciences, College of Bee Science and Biomedicine, Fujian Agriculture and Forestry University, Fuzhou, Fujian, China; Key Laboratory of Biopesticide and Chemical Biology (Ministry of Education), College of Plant Protection, Fujian Agriculture and Forestry University, Fuzhou, Fujian, China.
  • 4 Department of Biopharmaceutical Sciences, College of Bee Science and Biomedicine, Fujian Agriculture and Forestry University, Fuzhou, Fujian, China.
  • 5 Key Laboratory of Biopesticide and Chemical Biology (Ministry of Education), College of Plant Protection, Fujian Agriculture and Forestry University, Fuzhou, Fujian, China.
  • 6 Department of Biopharmaceutical Sciences, College of Bee Science and Biomedicine, Fujian Agriculture and Forestry University, Fuzhou, Fujian, China. Electronic address: linran@fafu.edu.cn.
  • 7 Guangdong Key Laboratory of Animal Conservation and Resource Utilization, Guangdong Public Laboratory of Wild Animal Conservation and Utilization, Institute of Zoology, Guangdong Academy of Sciences, Guangzhou, Guangdong, China. Electronic address: yaohl@giz.gd.cn.
PMID: 40048796 DOI: 10.1016/j.ejmech.2025.117461
Abstract

Allergic rhinitis (AR) is a non-infectious inflammatory disease and affects nearly half of the world's population currently, thus becoming a global health problem. In our study, a series of 1,2,4-triazole enamides were designed and used to evaluate the anti-inflammatory activity of AR. We found that compound 11g could significantly reduce the increased expression of interleukin-6 (IL-6), interleukin-1β (IL-1β) and tumor necrosis factor-α (TNF-α) in Raw264.7 cells induced by lipopolysaccharides (LPS), and inhibit the expression of inflammation through MAPK pathway and NF-κB pathway by influencing the expression of cannabinoid-1 receptor (CB1 R). In the AR mice model, 11g can significantly reduce the number of inflammatory cells in Nasal lavage fluids (NLF), showing a good effect on the treatment of AR. This study provides a new and effective candidate for treatment of AR.

Keywords

1,2,4-Triazole-enamides; Allergic rhinitis; Anti-inflammation; CB1 receptor; MAPK; NF-κB.

Figures
Products