Background: In this work, a wide spectrum of 5-aminomethylene barbituric/ thiobarbituric acid derivatives was synthesized and evaluated for their Jack bean urease inhibitory activity.

Methods: Among the synthesized compounds, 5-cyclohexylaminomethylene barbituric acid (3a) showed the most potent activity (IC50 = 25.8 μM), 4 times more potent than hydroxyurea (IC50 = 100.0 μM) and a similar activity to thiourea (IC50 = 22.0 μM), both being as the reference drugs.

Results and Conclusion: Also, results from docking studies were in good agreement with those obtained in in vitro assay.