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.

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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
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article

Synthesis of Paracetamol‐Appended Bis 1,2,3‐Triazole Analogues as Anti‐Inflammatory Agents

Vishnu Thumma, Jalapathi Pochampally, A. Kishore Kumar, Veerabhadraiah Mallikanti et al.
9 citations
ChemistrySelect
Click Chemistry and Applications
2.25
article

Synthesis of Paracetamol‐Appended Bis 1,2,3‐Triazole Analogues as Anti‐Inflammatory Agents

Vishnu Thumma, Jalapathi Pochampally, A. Kishore Kumar, Veerabhadraiah Mallikanti, Vineesha Bathini
article en
9 citations

Abstract

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.

ChemistrySelectVol. 9(42)
Osmania University (IN)
Clean water and sanitation
Openalex Percentile: Top 12%
Click Chemistry and Applications
2.25
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