A Synthesis, Antimicrobial Screening, Urease Inhibition and Molecular Docking Studies of 2-Arylimino-4-Thiazolidinone Derivatives synthesis, biological evaluation and docking studies
International Pharmacy Acta,
Vol. 8 No. 1 (2025),
6 April 2025
,
Page e12: 1-9
https://doi.org/10.22037/ipa.v8i1.48580
Abstract
A series of six new arylidene derivatives of 2-imino-4-thiazolidinone has been synthesised by the condensation of 2-arylimino-4-thiazolidinones with hydroxy-substituted aldehydes. All the compounds were characterised by IR, 1H NMR, 13C NMR, and mass spectrometry, and screened for antibacterial, antifungal, and urease-inhibitory potential. Almost all derivatives exhibited moderate to strong antibacterial and antifungal activity. Compounds 7 and 5 exhibited great potential with 17.0mm and 15.0mm zones of inhibition against Staphylococcus aureus, and compound 5 showed moderate potential against Candida glabrata with a 5.0mm zone of inhibition. The arylidene derivatives of 4-hydroxyphenylimino-4-thiazolidinone showed good urease inhibition activity with IC50 values ranging from 32.5 ± 1.16 µM to 46.6 ± 1.96 µM. All results were validated using docking studies, and the binding interactions of these compounds with the enzyme were assessed.
- HCV
- NS5B polymerase
- Thiazolone derivatives
- Molecular docking
- ADME/Tox
- Normal mode analysis
How to Cite
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