Find in Library
Search millions of books, articles, and more
Indexed Open Access Databases
Synthesis and in vitro activity tests of N-benzoyl-N’-phenylthiourea derivatives as macrophage migration inhibitory factor
oleh: Dini Kesuma, Galih S. Putra, Tegar A. Yuniarta, Farida Suhud, I G.A. Sumartha, Sawitri Boengas, Melanny I. Sulistyowaty, Tjie Kok
| Format: | Article |
|---|---|
| Diterbitkan: | GarVal Editorial Ltda. 2023-09-01 |
Deskripsi
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.