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Abstract <p>For the development of new anti-tubercular (TB) drugs, imidazopyridine-chalcone conjugates were synthesized. A combination of elemental and spectroscopy analysis was used for structural characterization of newly developed compounds. Anti-TB screening and cytotoxicity assays with Vero cells were conducted to evaluate the effectiveness of the synthesized compounds. It was found that few compounds were more effective than standard anti-TB drug pyrazinamide. Based on docking experiments performed on mycobacterium tuberculosis InhA bound to NITD-916 (PDB: 4R9S), certain compounds showed a greater affinity for protein binding. Moreover, the most active anti-TB compounds had outstanding safety profiles and exhibited high levels of interaction with the target protein. They may prove valuable as leads to new anti-TB treatments. The results clearly indicate that imidazopyridine-chalcone compounds may offer a good platform for developing effective antitubercular agents.</p>

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Design and Synthesis of Novel Imidazopyridine-Chalcone Hybrids As Potent Anti-TB Agents with Their Docking and Cytotoxicity Studies

  • 期刊论文

  • 发表日期：

    2025年9月1日

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  • Rajakumar Patil,
  • Dinesh S. Reddy,
  • Vidya G,
  • Hamzad Shanavaz,
  • Sashivinay Kumar Gaddam,
  • Nikhil Kadam,
  • Deepak Kasai

摘要

Abstract

For the development of new anti-tubercular (TB) drugs, imidazopyridine-chalcone conjugates were synthesized. A combination of elemental and spectroscopy analysis was used for structural characterization of newly developed compounds. Anti-TB screening and cytotoxicity assays with Vero cells were conducted to evaluate the effectiveness of the synthesized compounds. It was found that few compounds were more effective than standard anti-TB drug pyrazinamide. Based on docking experiments performed on mycobacterium tuberculosis InhA bound to NITD-916 (PDB: 4R9S), certain compounds showed a greater affinity for protein binding. Moreover, the most active anti-TB compounds had outstanding safety profiles and exhibited high levels of interaction with the target protein. They may prove valuable as leads to new anti-TB treatments. The results clearly indicate that imidazopyridine-chalcone compounds may offer a good platform for developing effective antitubercular agents.