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Synthesis of novel furan-based chalcone derivatives as anti-tuberculosis agents: in vitro , cytotoxicity assessment and in silico .

Loganathan Sumathi DhivyaKathiravan Muthu Kumaradoss
Published in: Future medicinal chemistry (2023)
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; IC 50 ) 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.
Keyphrases
  • mycobacterium tuberculosis
  • pulmonary tuberculosis
  • molecular docking
  • oxidative stress
  • oxide nanoparticles
  • human immunodeficiency virus
  • electronic health record
  • signaling pathway
  • human health
  • adverse drug