1,4-disubstituted 1h-1,2,3-triazoles for renal diseases: Studies of viability, anti-inflammatory, and antioxidant activities

Ching Yi Cheng*, Ashanul Haque, Ming Fa Hsieh, Syed Imran Hassan, Md Serajul Haque Faizi, Necmi Dege, Muhammad S. Khan

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

17 Citations (Scopus)


Inflammation is a hallmark of many metabolic diseases. We previously showed that ferrocene-appended 1H-1,2,3-triazole hybrids inhibit nitric oxide (NO) production in in vitro models of lipopolysaccharide-induced inflammation in the BV-2 cell. In the present study, we explored the viability, anti-inflammatory, and antioxidant potential of ferrocene-1H-1,2,3-triazole hybrids using biochemical assays in rat mesangial cells (RMCs). We found that, among all the ferrocene-1H-1,2,3-triazole hybrids, X2–X4 exhibited an antioxidant effect on mitochondrial free radicals. Among all the studied compounds, X4 demonstrated the best anti-inflammatory effect on RMCs. These results were supplemented by in silico studies including molecular docking with human cytosolic phospholipase A2 (cPLA2) and cyclooxygenase 2 (COX-2) enzymes as well as absorption, distribution, metabolism, excretion, and toxicity (ADMET) profiling. Besides, two new crystal structures of the compounds have also been reported. In addition, combining the results from the inducible nitric oxide synthase (iNOS), cPLA2, COX-2, and matrix metalloproteinase-9 (MMP-9) enzymatic activity analysis and NO production also confirmed this argument. Overall, the results of this study will be a valuable addition to the growing body of work on biological activities of triazole-based compounds.

Original languageEnglish
Article number3823
JournalInternational Journal of Molecular Sciences
Issue number11
Publication statusPublished - Jun 1 2020


  • Cytosolic phospholipase A (cPLA)
  • Inducible nitric oxide synthase (iNOS)
  • Matrix metalloproteinase-9 (MMP-9)
  • Prostaglandin E (PGE)
  • Tumor necrosis factor-α (TNF-α)

ASJC Scopus subject areas

  • Catalysis
  • Molecular Biology
  • Spectroscopy
  • Computer Science Applications
  • Physical and Theoretical Chemistry
  • Organic Chemistry
  • Inorganic Chemistry


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