Synthesis of 4-thiazolidinone analogs as potent in vitro anti-urease agents.

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 IC 50 values 1.73–69.65 μM, if compared with standard thiourea having IC 50 value of 21.25 ± 0.15 μM. Among the series, eight derivatives 3 , 6 , 8 , 10 , 15 , 17 , 19 , and 20 showed outstanding urease inhibitory potential with IC 50 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 ± 0.001 μM, 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.