Journal of Pharmacy & Pharmacognosy Research (Sep 2023)

Synthesis and in vitro activity tests of N-benzoyl-N’-phenylthiourea derivatives as macrophage migration inhibitory factor

  • Dini Kesuma,
  • Galih S. Putra,
  • Tegar A. Yuniarta,
  • Farida Suhud,
  • I G.A. Sumartha,
  • Sawitri Boengas,
  • Melanny I. Sulistyowaty,
  • Tjie Kok

DOI
https://doi.org/10.56499/jppres23.1657_11.5.902
Journal volume & issue
Vol. 11, no. 5
pp. 902 – 925

Abstract

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Context: The COVID-19 pandemic in 2020 resulted in widespread mortalities due to cytokine storms in the affected patients. Macrophage migration inhibitory factor (MIF) is one of the most interesting targets in developing anti-COVID-19 drugs. Some thiourea compounds have been identified as having potential as MIF inhibitors. Aims: To investigate MIF inhibitory activity of N-benzoyl-N’-phenylthiourea derivatives. Methods: The study consists of in-silico activity prediction of designed compounds using a molecular docking approach against MIF protein (PDB ID: 1LJT). Afterwards, the designed compounds were synthesized and tested in vitro using the tautomerase activity approach. Results: The molecular docking study showed that all designed compounds possess comparable docking scores to the native ligand of the protein. MIF Assay performed on compounds (1) and (2) indicated a decrease in tautomerase activity of the MIF target protein of only 10.1 and 6.2%, respectively, compared to the positive control. Conclusions: In silico results predicted better bioactivity against MIF protein, but the result does not translate to the in vitro assay, where two of the designed compounds possess only low inhibitory activity.

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