New 1,2,3‐Triazole‐Tethered Thiazolidinedione Derivatives: Synthesis, Bioevaluation and Molecular Docking Study

Abstract

In search of new active molecules, a small focused library of 1,2,3-triazoles based 2,4-thiazolidinedione derivatives has been efficiently prepared via the click chemistry approach. Several derivatives were exhibited excellent anti-inflammatory activity compared to the standard drug. Further, the synthesized compounds were found to have potential antioxidant activity. Furthermore, to rationalize the observed biological activity data, the molecular docking study has also been carried out against the active site of inflammation enzyme PPARγ, which revealed a significant correlation between the binding score and biological activity for these compounds. The results of the in vitro and in silico study suggest that the triazole incorporated 2,4-thiazolidinedione derivatives may possess the ideal structural requirements for the further development of novel therapeutic agents.

Graphical Abstract

Keywords:

• Click chemistry
• 1,2,3-triazoles
• anti-inflammatory activity
• antioxidant activity
• 2,4-thiazolidinedione

Acknowledgements

The authors M.H.S., D.D.S. and S.V.A. are very much grateful to the Council of Scientific and Industrial Research (CSIR), New Delhi for the award of Research Fellowship. Authors also thank Schrodinger Inc. for GLIDE software to perform the molecular docking studies.

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

Authors are thankful to the University Grants Commission and Department of Science & Technology, New Delhi for financial support under UGC-SAP and DST-FIST schemes.