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  • Title: Synthesis of 4-thiazolidinone analogs as potent in vitro anti-urease agents.
    Author: Rahim F, Zaman K, Ullah H, Taha M, Wadood A, Javed MT, Rehman W, Ashraf M, Uddin R, Uddin I, Asghar H, Khan AA, Khan KM.
    Journal: Bioorg Chem; 2015 Dec; 63():123-31. PubMed ID: 26520885.
    Abstract:
    4-Thiazolidinone analogs 1-20 were synthesized, characterized by (1)H NMR and EI-MS and investigated for urease inhibitory activity. All twenty (20) analogs exhibited varied degree of urease inhibitory potential with IC50 values 1.73-69.65μM, if compared with standard thiourea having IC50 value of 21.25±0.15μM. Among the series, eight derivatives 3, 6, 8, 10, 15, 17, 19, and 20 showed outstanding urease inhibitory potential with IC50 values of 9.34±0.02, 14.62±0.03, 8.43±0.01, 7.3±0.04, 2.31±0.002, 5.75±0.003, 8.81±0.005, and 1.73±0.001μM, respectively, which is better than the standard thiourea. The remaining analogs showed good to excellent urease inhibition. The binding interactions of these compounds were confirmed through molecular docking studies.
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