Synthesis of Novel Furan-Based Chalcone Derivatives As Anti-Tuberculosis Agents: In Vitro, Cytotoxicity Assessment and In Silico

Abstract

Background: The aim of the study is to identify a novel furan-based chalcone derivative as potent inhibitor against the H37Rv strain. Materials & methods: The in silico pharmacokinetic characteristics, toxicity tests, molecular modeling, chemical synthesis and minimum inhibitory concentration (MIC; IC₅₀) were carried out to evaluate the antitubercular potential of the synthesized furan-based chalcone analogues against H37Rv. Results & conclusion: Among the ten target compounds synthesized, DF02, DF05 and DF07 had MIC values of 1.6 μg/ml equivalent to isoniazid and DF10 showed MIC values of 3.25 μg/ml which is equipotent to pyrazinamide. All the other compounds had optimal concentrations 6.25–100 μg/ml against the H37Rv strain. Compounds DF02 and DF10 were further evaluated for cytotoxicity assay performed using HeLa cell lines.

Keywords:

• furan-based chalcone analogue
• H37Rv
• HeLa cell lines
• InhA
• molecular modeling

Supplementary data

To view the supplementary data that accompany this paper please visit the journal website at:www.tandfonline.com/doi/full/10.2217/epi-2016-0184

Acknowledgments

We would like to thank Research Council of SRM Institute of Science and Technology for their constant support.

Financial & competing interests disclosure

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending or royalties.

No writing assistance was utilized in the production of this manuscript.