Synthesis of Paracetamol‐Appended Bis 1,2,3‐Triazole Analogues as Anti‐Inflammatory Agents
Abstract Paracetamol‐based bis 1,2,3‐triazole analogues were synthesized involving copper‐catalyzed click chemistry protocol. The new compounds were characterized by 1 H NMR, 13 C NMR, and mass spectral techniques. All the compounds were evaluated for their in vitro anti‐inflammatory properties using diclofenac as standard reference. The compound 6b with chlorine and fluorine functions displayed outstanding activity with IC 50 values of 7.34 ± 0.45 µM and 7.84 ± 0.47 µM, respectively. Compound 6g with methyl and fluorine functions displayed best activity with IC 50 values of 9.34 ± 0.22 µM and 9.40 ± 0.35 µM, respectively. Compound 6i , 6k, 6f, 6a, 6e, 6h, 6j , and 6l exhibited promising activity with respect to diclofenac. Using PyRx tool, the molecular docking study against crystal structure of COX‐2 proved the binding efficacies with notable binding interactions.
Authors
- Vishnu Thumma (ORCID: https://orcid.org/0000-0001-6830-3671)
- Jalapathi Pochampally (ORCID: https://orcid.org/0000-0002-5419-6868)
- A. Kishore Kumar (ORCID: https://orcid.org/0000-0002-5621-5997)
- Veerabhadraiah Mallikanti
- Vineesha Bathini
Institutions
- Osmania University (IN)
Publication Details
- Journal
- ChemistrySelect
- Published
- 2024-11-01
- DOI
- https://doi.org/10.1002/slct.202403390
- Citations
- 9
- Primary Topic
- Click Chemistry and Applications
- Type
- article
- Field-Weighted Citation Impact
- 2.25