Hydrazones were considered as significant substrates in drug discovery process. Therefore, a series of some new 1-(4-(1-(2-(4-substitutedphenyl)hydrazono)ethyl)phenyl)-3-(4-nitrophenyl)urea derivatives (2-8) were synthesized as potential urease inhibitory agents. The synthesized compounds were characterized by FTIR, ¹H NMR, 13C NMR, and elemental analysis (C, H, N). All compounds were evaluated in vitro for urease inhibitory potential. Among synthesized compounds, 8, 7, 6, and 4 showed excellent activities (IC50) i.e. 10.13±0.40, 12.15±0.22, 17.81±0.36, and 22.95±0.47 µM, respectively. This study has culminated in the identification of some compounds which can serve as leads for new potent urease inhibitors.